Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTZAYWL)

• DTT Name: Estrogen receptor (ESR)
• Synonyms: Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER
• Gene Name: ESR1
• DTT Type: Successful target; [1]
• Related Disease:
  Acne vulgaris [ICD-11: ED80]
  Acquired prion disease [ICD-11: 8E01]
  Adrenal cancer [ICD-11: 2D11]
  Breast cancer [ICD-11: 2C60-2C6Y]
  Contraceptive management [ICD-11: QA21]
  Dyspareunia [ICD-11: GA12]
  Female infertility [ICD-11: GA31]
  Low bone mass disorder [ICD-11: FB83]
  Male infertility [ICD-11: GB04]
  Menopausal disorder [ICD-11: GA30]
  Menstrual cycle bleeding disorder [ICD-11: GA20]
  Pituitary gland disorder [ICD-11: 5A60-5A61]
  Skeletal anomaly [ICD-11: LD24]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]
  Vaginitis [ICD-11: GA02]
• BioChemical Class: Nuclear hormone receptor
• UniProt ID: ESR1_HUMAN
• TTD ID: T89534
• Sequence:
  MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
  EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
  LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
  ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
  RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
  SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
  AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
  MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
  KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
  LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
• Function: Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full-length receptor. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1.
• KEGG Pathway:
  Estrogen signaling pathway (hsa04915)
  Prolactin signaling pathway (hsa04917)
  Thyroid hormone signaling pathway (hsa04919)
  Endocrine and other factor-regulated calcium reabsorption (hsa04961)
  Proteoglycans in cancer (hsa05205)
• Reactome Pathway:
  Nuclear Receptor transcription pathway (R-HSA-383280)
  Nuclear signaling by ERBB4 (R-HSA-1251985)

Molecular Interaction Atlas (MIA) of This DTT

36 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARZOXIFENE	DMOKCVI	Breast cancer	2C60-2C65	Approved	[2]
Bazedoxifene	DMY85QW	Osteopetrosis	LD24.10	Approved	[3], [4]
Cenestin	DMXQS7K	Menopause symptom	GA30.0	Approved	[5], [4], [6]
Clomifene	DMKI7RB	Female infertility	GA31.Z	Approved	[7]
Clomiphene citrate	DMS51VC	Female infertility	GA31.Z	Approved	[8]
Conjugated estrogens a	DMTPIZC	Hormone replacement therapy	8E01	Approved	[9]
Conjugated estrogens b	DMU7SF8	Hormone replacement therapy	8E01	Approved	[10], [9]
Cyclofenil	DMT5RMB	Infertility	GB04	Approved	[11], [4]
Danazol	DML8KTN	Menorrhagia	GA20.50	Approved	[12]
Dienestrol	DMBSXI0	Atrophic vaginitis	GA30.2	Approved	[13]
Diethylstilbestrol	DMN3UXQ	Gonorrheal vaginitis	GA02	Approved	[14]
Esterified estrogens	DM9KZDO	Breast cancer	2C60-2C65	Approved	[15], [4]
Estradiol	DMUNTE3	Breast cancer	2C60-2C65	Approved	[16]
Estradiol acetate	DM07U2A	Hormone replacement therapy	8E01	Approved	[8]
Estradiol cypionate	DM27Z5T	Hormone replacement therapy	8E01	Approved	[8]
Estradiol valerate	DM8MC6O	Hormone replacement therapy	8E01	Approved	[8]
Estriol	DMOEM2I	Hormone deficiency	5A61.1	Approved	[16]
Estrogen	DMGY0UT	Menopause symptom	GA30.0	Approved	[17]
Estrone	DM5T6US	Menopausal and postmenopausal disorder	GA30	Approved	[16]
Estropipate	DMRMDWA	Hypogonadism	5A61.0	Approved	[18], [4]
Ethinyl estradiol	DMODJ40	Female hypogonadism	GA30.6	Approved	[19], [16]
Fosfestrol	DMD072M	Solid tumour/cancer	2A00-2F9Z	Approved	[20], [21]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[1]
Gestrinone	DMP0OVQ	Breast cancer	2C60-2C65	Approved	[9]
Lasofoxifene	DMHA18P	Osteoporosis	FB83.0	Approved	[22]
Levormeloxifene	DM2XVNI	Breast cancer	2C60-2C65	Approved	[23], [4]
Mestranol	DMG3F94	Contraception	QA21	Approved	[24]
Mitotane	DMU1GX0	Adrenocortical carcinoma	2D11.Z	Approved	[25], [26]
Nomegestrol acetate	DMRJ7D1	Breast cancer	2C60-2C65	Approved	[27], [28], [4]
Ospemifene	DMC4GEI	Dyspareunia	GA12	Approved	[29]
Premarin/Trimegestone	DMYQVGN	Menopause symptom	GA30.0	Approved	[30], [4]
Promestriene	DMU92F8	Acne vulgaris	ED80	Approved	[31], [4]
Quinestrol	DMJ6H1Z	Breast cancer	2C60-2C65	Approved	[32]
Raloxifene	DMDKF3M	Osteoporosis	FB83.0	Approved	[33]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[34], [35]
Toremifene	DMQYUWG	Breast cancer	2C60-2C65	Approved	[36]

28 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acolbifene	DM3UQ9K	Breast cancer	2C60-2C65	Phase 3	[37]
NPC-01	DMMC3Y8	Dysmenorrhea	GA34.3	Phase 3	[38]
Premarin/Pravachol	DMLSOB7	Hyperlipidaemia	5C80	Phase 3	[39]
RAD-1901	DM8RLJ5	Breast cancer	2C60-2C65	Phase 3	[40]
Synthetic conjugated estrogen	DMRUEKC	Vaginal disease	GA1Y	Phase 3	[41], [4]
Trimegestone/ethinyl estradiol	DMS57DJ	Contraception	QA21	Phase 3	[42]
TZTX-001	DM71ZL6	Endometriosis	GA10	Phase 3	[43]
Afimoxifene	DMFORDT	Breast cancer	2C60-2C65	Phase 2	[33]
ARN-810	DML3PJF	Breast cancer	2C60-2C65	Phase 2	[44]
AZD9833	DMQOTHP	ER-positive breast cancer	2C60-2C65	Phase 2	[45]
Endoxifen	DMTX8IZ	Breast cancer	2C60-2C65	Phase 2	[33]
Estetrol	DMTB63Q	Autoimmune diabetes	5A10	Phase 2	[46]
GTx-758	DMDWYZS	Prostate cancer	2C82.0	Phase 2	[47]
Icaritin	DMGHQ37	Breast cancer	2C60-2C65	Phase 2	[48]
SR 16234	DMRFO34	Breast cancer	2C60-2C65	Phase 2	[49]
H3B-6545	DMIFCY2	Breast cancer	2C60-2C65	Phase 1/2	[50]
OP-1250	DMIU26T	Breast cancer	2C60-2C65	Phase 1/2	[51]
ZN-c5	DMVG4OC	Breast cancer	2C60-2C65	Phase 1/2	[52]
ATD transdermal gel	DMIMH8L	Contraception	QA21	Phase 1	[33]
Azd9496	DMPMDTH	Breast cancer	2C60-2C65	Phase 1	[50]
CC-8490	DMXUT3Z	Brain cancer	2A00	Phase 1	[53]
CHF-4227	DMTE18G	Osteoporosis	FB83.0	Phase 1	[54]
D-0502	DMGA1DS	Breast cancer	2C60-2C65	Phase 1	[55]
G1T-48	DMRGP72	Breast cancer	2C60-2C65	Phase 1	[56]
LY3484356	DMY8W3S	Breast cancer	2C60-2C65	Phase 1	[57]
SCO-120	DMB1MZS	Breast cancer	2C60-2C65	Phase 1	[58]
TTC-352	DM7CHZ2	Breast cancer	2C60-2C65	Phase 1	[50]
TTC-352	DM7E6V2	Metastatic melanoma	2E2Z	Phase 1	[59]

21 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bithionol	DMPJKRL	Trematode infection	1F8Y	Withdrawn from market	[60]
Chlorotrianisene	DMSV2WZ	Menopause symptom	GA30.0	Withdrawn from market	[61]
HEXESTROL	DM9AGWQ	Irregularities	N.A.	Withdrawn from market	[62]
EM-800	DM5JUW0	Estrogen deficiency	FB83.0Y	Discontinued in Phase 3	[63]
Idoxifene	DMRXUY7	Breast cancer	2C60-2C65	Discontinued in Phase 3	[64]
IoGen	DMVL8PB	Pain	MG30-MG3Z	Discontinued in Phase 3	[33]
Miproxifene	DMMZO8X	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 3	[65]
Droloxifene	DM9JPUD	Breast cancer	2C60-2C65	Discontinued in Phase 2	[66]
ERA-923	DM6NTAS	Breast cancer	2C60-2C65	Discontinued in Phase 2	[67], [68]
NP-50301	DMPMR2I	Eye disorder	9A01-9A0Z	Discontinued in Phase 2	[69]
Panomifene	DME4RSI	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[70]
SERM-3339	DMSLP2O	Osteoporosis	FB83.0	Discontinued in Phase 2	[71]
SR-90067	DMROKDM	Hormone deficiency	5A61.1	Discontinued in Phase 2	[72]
HE2100	DMCP2KH	Thrombocytopenia	3B64	Discontinued in Phase 1	[73]
HRT	DMQYWAH	Estrogen deficiency	FB83.0Y	Discontinued in Phase 1	[74]
MX-4509	DMC4RK7	Neurological disorder	6B60	Discontinued in Phase 1	[75]
ICI-164384	DMYN3WG	Breast cancer	2C60-2C65	Terminated	[78]
LY-117018	DMUHG0F	N. A.	N. A.	Terminated	[79]
Tamoxifen methyl iodide	DM54V0X	N. A.	N. A.	Terminated	[80]
Zindoxifene	DM81DJV	Breast cancer	2C60-2C65	Terminated	[81]
ZK-119010	DMKFYDE	Carcinoma	2A00-2F9Z	Terminated	[82]

6 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BN-AA-003-NY	DMCPQJ9	Estrogen deficiency	FB83.0Y	Preclinical	[76]
BN-AO-014	DMVMY4X	Atrophy	9A2Y-9C40	Preclinical	[76]
BN-CB-045	DMBPTDC	Female sexual arousal dysfunction	HA01.1	Preclinical	[76]
BN-DF-037	DMFNLE6	Osteoporosis	FB83.0	Preclinical	[76]
BN-GU-005-DHP	DM0PJU9	Arthralgia	ME82	Preclinical	[76]
BN-OD-026	DM8WDAL	Solid tumour/cancer	2A00-2F9Z	Preclinical	[77]

195 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol	DM9RF1T	Discovery agent	N.A.	Investigative	[83]
1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol	DMKJBRZ	Discovery agent	N.A.	Investigative	[84]
1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol	DM2T4NL	Discovery agent	N.A.	Investigative	[84]
1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL	DM0MGFQ	Discovery agent	N.A.	Investigative	[84]
1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol	DM8BC1M	Discovery agent	N.A.	Investigative	[84]
17-METHYL-17-ALPHA-DIHYDROEQUILENIN	DMKUGH1	Discovery agent	N.A.	Investigative	[85]
2,3-diphenyl-1H-indole	DMC3UYH	Discovery agent	N.A.	Investigative	[86]
2,4-Dibenzylamino-6-isopentylpyrimidine	DMQ385U	Discovery agent	N.A.	Investigative	[87]
2,4-diisobutylamino-6-isopentylpyrimidine	DM0URFY	Discovery agent	N.A.	Investigative	[87]
2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol	DMWDV71	Discovery agent	N.A.	Investigative	[88]
2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol	DMJM5VW	Discovery agent	N.A.	Investigative	[88]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol	DMBONUV	Discovery agent	N.A.	Investigative	[88]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol	DM3B6IN	Discovery agent	N.A.	Investigative	[88]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol	DMNTHK5	Discovery agent	N.A.	Investigative	[88]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol	DM50FW1	Discovery agent	N.A.	Investigative	[88]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol	DMZCE18	Discovery agent	N.A.	Investigative	[89]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol	DMIGXRJ	Discovery agent	N.A.	Investigative	[89]
2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol	DMUGHF6	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol	DM4N0LB	Discovery agent	N.A.	Investigative	[90]
2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol	DM81G2U	Discovery agent	N.A.	Investigative	[90]
2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol	DMFWOMY	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol	DMY0I8P	Discovery agent	N.A.	Investigative	[91]
2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol	DMCNITS	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol	DMQ2KPI	Discovery agent	N.A.	Investigative	[91]
2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol	DMUB7KH	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol	DMND63Z	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol	DMONT2D	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol	DM2F6U3	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-benzooxazol-5-ol	DMMUNA7	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-benzooxazol-6-ol	DM31MY0	Discovery agent	N.A.	Investigative	[88]
2-(4-Hydroxy-phenyl)-quinolin-6-ol	DMCWFUZ	Discovery agent	N.A.	Investigative	[90]
2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL	DMN6S3F	Discovery agent	N.A.	Investigative	[88]
2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol	DMW6L38	Discovery agent	N.A.	Investigative	[89]
2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol	DMB3JG0	Discovery agent	N.A.	Investigative	[88]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol	DMXAVHT	Discovery agent	N.A.	Investigative	[88]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol	DM3GQN2	Discovery agent	N.A.	Investigative	[88]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol	DM715EC	Discovery agent	N.A.	Investigative	[88]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol	DMANHOT	Discovery agent	N.A.	Investigative	[88]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE	DMNQL17	Discovery agent	N.A.	Investigative	[85]
2-Naphthalen-1-yl-benzooxazol-6-ol	DMBI6U9	Discovery agent	N.A.	Investigative	[88]
2-phenyl-1,2'-spirobi[1H-indene]-5'-ol	DMP8G3C	Discovery agent	N.A.	Investigative	[89]
3'-Methoxy-4'Hydroxyclomiphene	DMG1T6H	Discovery agent	N.A.	Investigative	[92]
3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one	DMIFJRS	Discovery agent	N.A.	Investigative	[93]
3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one	DMW0B4H	Discovery agent	N.A.	Investigative	[93]
3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol	DMD24EW	Discovery agent	N.A.	Investigative	[88]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol	DMXZ9T6	Discovery agent	N.A.	Investigative	[88]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol	DMYLDFG	Discovery agent	N.A.	Investigative	[88]
3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one	DMS5N6Y	Discovery agent	N.A.	Investigative	[94]
3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one	DMH75AO	Discovery agent	N.A.	Investigative	[94]
3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol	DMPRBLH	Discovery agent	N.A.	Investigative	[88]
3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol	DM5H9QT	Discovery agent	N.A.	Investigative	[88]
3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL	DM3R8OM	Discovery agent	N.A.	Investigative	[85]
3-chloro-4-(4-hydroxyphenyl)salicylaldoxime	DMER4U1	Discovery agent	N.A.	Investigative	[95]
3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL	DMEWAVM	Discovery agent	N.A.	Investigative	[85]
3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one	DM3H56L	Discovery agent	N.A.	Investigative	[93]
3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol	DMPTI1Z	Discovery agent	N.A.	Investigative	[96]
4',5,7-trihydroxy-6,8-dimethylisoflavone	DM1RM3H	Discovery agent	N.A.	Investigative	[97]
4,10-dimethyl-6H-benzo[c]chromene-3,8-diol	DMB5RJK	Discovery agent	N.A.	Investigative	[93]
4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol	DM6N98E	Discovery agent	N.A.	Investigative	[93]
4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol	DM14VI3	Discovery agent	N.A.	Investigative	[93]
4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol	DMYN25U	Discovery agent	N.A.	Investigative	[93]
4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol	DMFECXI	Discovery agent	N.A.	Investigative	[93]
4,7-dimethyl-6H-benzo[c]chromene-3,8-diol	DM67Z81	Discovery agent	N.A.	Investigative	[93]
4-(1,2-Diphenyl-but-1-enyl)-phenol	DMJDW50	Discovery agent	N.A.	Investigative	[98]
4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol	DMNV9H5	Discovery agent	N.A.	Investigative	[99]
4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol	DMS1OYA	Discovery agent	N.A.	Investigative	[99]
4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol	DM3NEYB	Discovery agent	N.A.	Investigative	[99]
4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol	DMFQZOI	Discovery agent	N.A.	Investigative	[86]
4-(2-phenyl-1H-indol-3-yl)phenol	DMCPSE9	Discovery agent	N.A.	Investigative	[86]
4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol	DMR3T2D	Discovery agent	N.A.	Investigative	[86]
4-(3-phenyl-1H-indol-2-yl)phenol	DMEJF6V	Discovery agent	N.A.	Investigative	[86]
4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol	DM1EANV	Discovery agent	N.A.	Investigative	[88]
4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL	DMHGRPB	Discovery agent	N.A.	Investigative	[85]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol	DM38YZ4	Discovery agent	N.A.	Investigative	[88]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol	DM07NT9	Discovery agent	N.A.	Investigative	[88]
4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol	DMUXZOM	Discovery agent	N.A.	Investigative	[99]
4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol	DM0X5SY	Discovery agent	N.A.	Investigative	[99]
4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol	DMEYUH0	Discovery agent	N.A.	Investigative	[99]
4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol	DMX2K8R	Discovery agent	N.A.	Investigative	[99]
4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol	DM1UG2A	Discovery agent	N.A.	Investigative	[88]
4-benzyl-2,6-diisobutylamino-pyrimidine	DM2Q0VB	Discovery agent	N.A.	Investigative	[87]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol	DMPSRAC	Discovery agent	N.A.	Investigative	[90]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol	DMKJ18X	Discovery agent	N.A.	Investigative	[90]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol	DMTIY89	Discovery agent	N.A.	Investigative	[90]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol	DMXLZAT	Discovery agent	N.A.	Investigative	[90]
4-hydroxy-N,N-diphenylbenzenesulfonamide	DMXPQ5H	Discovery agent	N.A.	Investigative	[100]
4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide	DMVAP9U	Discovery agent	N.A.	Investigative	[100]
4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide	DM8XOJC	Discovery agent	N.A.	Investigative	[100]
4-hydroxy-N-phenyl-N-propylbenzenesulfonamide	DM5TU98	Discovery agent	N.A.	Investigative	[100]
4-Naphthalen-2-yl-phenol	DMKPNSH	Discovery agent	N.A.	Investigative	[84]
4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol	DMW1IXY	Discovery agent	N.A.	Investigative	[101]
4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol	DMTL6ES	Discovery agent	N.A.	Investigative	[101]
4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol	DMTHG0Y	Discovery agent	N.A.	Investigative	[101]
4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol	DMR7GP6	Discovery agent	N.A.	Investigative	[101]
4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol	DMTMLXU	Discovery agent	N.A.	Investigative	[98]
4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol	DM30421	Discovery agent	N.A.	Investigative	[98]
4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol	DMWHKLA	Discovery agent	N.A.	Investigative	[98]
4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol	DMH1I32	Discovery agent	N.A.	Investigative	[98]
4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol	DM4BFPE	Discovery agent	N.A.	Investigative	[98]
4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol	DMS0HV6	Discovery agent	N.A.	Investigative	[101]
5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol	DM2YL0T	Discovery agent	N.A.	Investigative	[90]
5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol	DMCFIZN	Discovery agent	N.A.	Investigative	[88]
5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol	DMXNPSB	Discovery agent	N.A.	Investigative	[90]
5-hydroxy-2-phenylisoindoline-1,3-dione	DMLZKNF	Discovery agent	N.A.	Investigative	[102]
6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol	DMRU963	Discovery agent	N.A.	Investigative	[84]
6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol	DMFALTY	Discovery agent	N.A.	Investigative	[84]
6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol	DMTPAMS	Discovery agent	N.A.	Investigative	[84]
6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol	DM6Q3M7	Discovery agent	N.A.	Investigative	[84]
6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol	DMKJOL6	Discovery agent	N.A.	Investigative	[84]
6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol	DM4YP3Q	Discovery agent	N.A.	Investigative	[84]
6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol	DMAJEDG	Discovery agent	N.A.	Investigative	[84]
6-(3-Hydroxy-phenyl)-naphthalen-1-ol	DMMHRVO	Discovery agent	N.A.	Investigative	[84]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol	DMH8WA2	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol	DMYM3EW	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol	DMYEIRH	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol	DMBG5Y8	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol	DMGLT0N	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol	DMGC84U	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol	DMI6UVN	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-naphthalen-1-ol	DM2V9XI	Discovery agent	N.A.	Investigative	[84]
6-(4-Hydroxy-phenyl)-naphthalen-2-ol	DM3L2OI	Discovery agent	N.A.	Investigative	[90]
6-butyl-2,4-dipropylaminopyrimidine	DM46GLQ	Discovery agent	N.A.	Investigative	[87]
6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol	DMLMOC0	Discovery agent	N.A.	Investigative	[88]
6-ethyl-2,4-diisobutylaminopyrimidine	DMBMRUI	Discovery agent	N.A.	Investigative	[87]
6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol	DMOGETD	Discovery agent	N.A.	Investigative	[93]
6-Phenyl-naphthalen-2-ol	DMEYOF7	Discovery agent	N.A.	Investigative	[84]
7-(3-Hydroxy-phenyl)-naphthalen-2-ol	DM2I91C	Discovery agent	N.A.	Investigative	[84]
7-(4-Hydroxy-phenyl)-naphthalen-2-ol	DMM9IXB	Discovery agent	N.A.	Investigative	[84]
7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol	DMSRQ1L	Discovery agent	N.A.	Investigative	[88]
7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol	DMA8DXG	Discovery agent	N.A.	Investigative	[91]
7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol	DMQ8BIX	Discovery agent	N.A.	Investigative	[88]
7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol	DM38HKE	Discovery agent	N.A.	Investigative	[91]
7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one	DM2MIJY	Discovery agent	N.A.	Investigative	[94]
7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol	DMUMN4B	Discovery agent	N.A.	Investigative	[88]
7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol	DM92EG5	Discovery agent	N.A.	Investigative	[88]
7-Phenyl-naphthalen-2-ol	DM1WJFR	Discovery agent	N.A.	Investigative	[84]
8-(2,2-dimethylpropyl)naringenin	DMV5FZO	Discovery agent	N.A.	Investigative	[103]
8-(2-methylpropyl)naringenin	DMQUZSJ	Discovery agent	N.A.	Investigative	[103]
8-(3-methylbutyl)naringenin	DM2VAJE	Discovery agent	N.A.	Investigative	[103]
8-benzylnaringenin	DMKHF87	Discovery agent	N.A.	Investigative	[103]
8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol	DMB76ZN	Discovery agent	N.A.	Investigative	[84]
8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol	DMGJ3L6	Discovery agent	N.A.	Investigative	[84]
8-methylnaringenin	DMK63P2	Discovery agent	N.A.	Investigative	[103]
8-n-heptylnaringenin	DMWMVI3	Discovery agent	N.A.	Investigative	[103]
8-n-nonylnaringenin	DMC2JLQ	Discovery agent	N.A.	Investigative	[103]
8-n-pentylnaringenin	DMRDOP0	Discovery agent	N.A.	Investigative	[103]
8-n-propylnaringenin	DMDOW5S	Discovery agent	N.A.	Investigative	[103]
8-n-undecylnaringenin	DMXURM8	Discovery agent	N.A.	Investigative	[103]
BROUSSONIN A	DMXFN6H	Discovery agent	N.A.	Investigative	[104]
Carboron Cluster with phenol	DMCNV68	Discovery agent	N.A.	Investigative	[105]
Coumestrol	DM40TBU	Discovery agent	N.A.	Investigative	[106]
CP-394531	DMDPH3W	Discovery agent	N.A.	Investigative	[107]
CP-409069	DM1U6P7	Discovery agent	N.A.	Investigative	[107]
Daidzein	DMRFTJX	Discovery agent	N.A.	Investigative	[97]
DIHYDRORALOXIFENE	DM70OIC	Discovery agent	N.A.	Investigative	[108]
Doxorubicin-Formaldehyde Conjugate	DMJF6AQ	Discovery agent	N.A.	Investigative	[109]
EFFUSOL	DMXZRND	Discovery agent	N.A.	Investigative	[93]
Estriol E3	DMNXO9C	Multiple sclerosis	8A40	Investigative	[110]
Geldanamycin-estradiol hybrid	DMUSJ96	Discovery agent	N.A.	Investigative	[111]
GSK-5182	DMNGEAY	Discovery agent	N.A.	Investigative	[112]
GW7604	DMCA4RM	Discovery agent	N.A.	Investigative	[113]
JNJ-17148066	DMJ1DE9	Discovery agent	N.A.	Investigative	[114]
JNJ-19398990	DM94IJC	Discovery agent	N.A.	Investigative	[114]
JNJ-26529126	DMK6TVN	Discovery agent	N.A.	Investigative	[114]
JNJ-26529152	DMBZ7MA	Discovery agent	N.A.	Investigative	[114]
LTERHKILHRLLQEGSPSD	DMDU6F4	Discovery agent	N.A.	Investigative	[115]
methyl-piperidino-pyrazole	DMKTOPJ	Discovery agent	N.A.	Investigative	[116]
MPrP	DMWUK9G	Discovery agent	N.A.	Investigative	[117]
N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine	DMLU27Y	Discovery agent	N.A.	Investigative	[87]
N-allyl-4-hydroxy-N-phenylbenzenesulfonamide	DMZQUMB	Discovery agent	N.A.	Investigative	[100]
N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide	DM5TPEJ	Discovery agent	N.A.	Investigative	[100]
N-butyl-4-hydroxy-N-phenylbenzenesulfonamide	DMH5GW6	Discovery agent	N.A.	Investigative	[100]
N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide	DMCDBM5	Discovery agent	N.A.	Investigative	[100]
N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide	DMHY35A	Discovery agent	N.A.	Investigative	[100]
Nafoxidine	DM0FROP	Discovery agent	N.A.	Investigative	[118]
Org-37663	DM3EZDG	Discovery agent	N.A.	Investigative	[119]
propylpyrazoletriol	DMTCP8K	Discovery agent	N.A.	Investigative	[120]
R,R-THC	DM4URMA	Discovery agent	N.A.	Investigative	[121]
RG6046	DMGYWIK	Breast cancer	2C60-2C65	Investigative	[4]
SERMs	DM4ZYKV	Solid tumour/cancer	2A00-2F9Z	Investigative	[33]
SNG-163	DMOLQNK	Solid tumour/cancer	2A00-2F9Z	Investigative	[33]
SNG-8006	DMCT02Q	Osteoporosis	FB83.0	Investigative	[33]
SNG-8023	DM6O9DQ	Breast cancer	2C60-2C65	Investigative	[33]
SNG-8033	DM0W54R	leukaemia	2A60-2B33	Investigative	[33]
SOPHORAFLAVANONE B	DMUVKX5	Discovery agent	N.A.	Investigative	[103]
STX	DM7LZJ3	Estrogen deficiency	FB83.0Y	Investigative	[33]
Tamoxifen butyl bromide	DMBKL5O	Discovery agent	N.A.	Investigative	[80]
Tamoxifen ethyl bromide	DM76BXY	Discovery agent	N.A.	Investigative	[80]
Tamoxifen isopropyl bromide	DMBKWUZ	Discovery agent	N.A.	Investigative	[80]
Trans-hydroxytamoxifen	DMXS8LN	Discovery agent	N.A.	Investigative	[116]
TSERaM	DM6JF7T	Menopause symptom	GA30.0	Investigative	[33]
WAY-169916	DM94KWA	Discovery agent	N.A.	Investigative	[99]
WAY200070	DMBHXTL	Discovery agent	N.A.	Investigative	[88]
ZK-164015	DMROWV8	Discovery agent	N.A.	Investigative	[122]
[1,1':2',1'']Terphenyl-4'-carbaldehyde oxime	DMFXA8P	Discovery agent	N.A.	Investigative	[123]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Neuroectodermal tumour	2C82	Nervous tissue	2.05E-08	-0.08	-0.31
Prostate cancer	2C82	Prostate	9.80E-01	-0.11	-0.2
Breast cancer	2C82	Breast tissue	5.93E-18	0.18	0.37
Osteoporosis	FA20	Bone marrow	2.98E-01	-0.07	-0.28
Acute myelocytic leukaemia	2C82	Bone marrow	2.62E-01	-7.10E-04	-4.57E-03

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