Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DT3D8F0)

• DTP Name: Organic anion transporting polypeptide 1B1 (SLCO1B1)
• Gene Name: SLCO1B1
• UniProt ID: Q9Y6L6 (SO1B1_HUMAN)
• VARIDT ID: DTD0008
• Synonyms: LST-1; LST1; Liver-specific organic anion transporter 1; OATP-2; OATP-C; OATP1B1; OATP2; OATPC; SLC21A6; SLCO1B1; Sodium-independent organic anion-transporting polypeptide 2; Solute carrier family 21 member 6; Solute carrier organic anion transporter family member 1B1
• DTP Family: Organo Anion Transporter (OAT) Family
• Tissue Specificity: High expressed in sinusoidal (basolateral) membrane of hepatocytes, and is expressed uniformly throughout the lobules
• Sequence:
  MDQNQHLNKTAEAQPSENKKTRYCNGLKMFLAALSLSFIAKTLGAIIMKSSIIHIERRFE
  ISSSLVGFIDGSFEIGNLLVIVFVSYFGSKLHRPKLIGIGCFIMGIGGVLTALPHFFMGY
  YRYSKETNINSSENSTSTLSTCLINQILSLNRASPEIVGKGCLKESGSYMWIYVFMGNML
  RGIGETPIVPLGLSYIDDFAKEGHSSLYLGILNAIAMIGPIIGFTLGSLFSKMYVDIGYV
  DLSTIRITPTDSRWVGAWWLNFLVSGLFSIISSIPFFFLPQTPNKPQKERKASLSLHVLE
  TNDEKDQTANLTNQGKNITKNVTGFFQSFKSILTNPLYVMFVLLTLLQVSSYIGAFTYVF
  KYVEQQYGQPSSKANILLGVITIPIFASGMFLGGYIIKKFKLNTVGIAKFSCFTAVMSLS
  FYLLYFFILCENKSVAGLTMTYDGNNPVTSHRDVPLSYCNSDCNCDESQWEPVCGNNGIT
  YISPCLAGCKSSSGNKKPIVFYNCSCLEVTGLQNRNYSAHLGECPRDDACTRKFYFFVAI
  QVLNLFFSALGGTSHVMLIVKIVQPELKSLALGFHSMVIRALGGILAPIYFGALIDTTCI
  KWSTNNCGTRGSCRTYNSTSFSRVYLGLSSMLRVSSLVLYIILIYAMKKKYQEKDINASE
  NGSVMDEANLESLNKNKHFVPSAGADSETHC
• Function: This transporter involved in the clearance of bile acids and organic anions from the liver. Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine.
• Endogenous Substrate(s): Bisglucuronosyl bilirubin; Cholate; Dehydroepiandrosterone sulfate; Eicosanoids; Monoglucuronosyl bilirubin; Thyroid hormones; Tauroursodeoxycholate
• TCDB ID: 2.A.60.1.5
• Gene ID: 10599
• Reactome Pathway:
  Heme degradation (R-HSA-189483)
  Defective SLCO1B1 causes hyperbilirubinemia, Rotor type (HBLRR) (R-HSA-5619110)
  Transport of organic anions (R-HSA-879518)
  Atorvastatin ADME (R-HSA-9754706)
  Recycling of bile acids and salts (R-HSA-159418)

Molecular Interaction Atlas (MIA) of This DTP

64 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acocantherin	DM7JT24	Atrial fibrillation	BC81.3	Approved	[2]
Atorvastatin	DMF28YC	Cardiovascular disease	BA00-BE2Z	Approved	[3]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[4]
Bosentan	DMIOGBU	Pulmonary arterial hypertension	BB01.0	Approved	[5]
Bromfenac	DMKB79O	Postoperative inflammation	1A00-CA43.1	Approved	[6]
Caspofungin	DMGQIPT	Fungal infection	1F29-1F2F	Approved	[7]
Cefazolin	DMPDYFR	Bacterial infection	1A00-1C4Z	Approved	[7]
Cefditoren	DMSUVM1	Bacterial infection	1A00-1C4Z	Approved	[7]
Cefoperazone	DM53PV8	Bacterial infection	1A00-1C4Z	Approved	[7]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[8]
Cholic acid	DM7OKQV	Peroxisomal disorder	5C57	Approved	[7]
Cilostazol	DMZMSCT	Intermittent claudication	BD40.00	Approved	[9]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[10]
Darunavir	DMN3GCH	Human immunodeficiency virus infection	1C62	Approved	[7]
Dasatinib	DMJV2EK	Chronic myelogenous leukaemia	2A20.0	Approved	[10]
Dehydroepiandrosterone sulfate	DM4Q80H	Dyspareunia	GA12	Approved	[7]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[7]
Docetaxel	DMDI269	Solid tumour/cancer	2A00-2F9Z	Approved	[8]
Eluxadoline	DMYZ0P1	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[11]
Enalapril	DMNFUZR	Hypertension	BA00-BA04	Approved	[12]
Entacapone	DMLBVKQ	Parkinson disease	8A00.0	Approved	[6]
Estrone sulfate	DMVBIZL	Menopausal and postmenopausal disorder	GA30	Approved	[13]
Etoposide	DMNH3PG	Solid tumour/cancer	2A00-2F9Z	Approved	[14]
Ezetimibe	DM7A8TW	Hypercholesterolaemia	5C80.0	Approved	[15]
Fluorescein	DMQTFAO	Ocular disease	1F00.1Z	Approved	[6]
Fluvastatin	DM4MDJY	Hypercholesterolaemia	5C80.0	Approved	[16]
Gadobenate dimeglumine	DM4VAOG	Schizophrenia	6A20	Approved	[17]
Gefitinib	DM15F0X	Solid tumour/cancer	2A00-2F9Z	Approved	[10]
Hydroxyurea	DMOQVU9	Chronic myelogenous leukaemia	2A20.0	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[10]
Levothyroxine	DMHN027	Hypothyroidism	5A00	Approved	[19]
Liothyronine	DM6IR3P	Hypothyroidism	5A00	Approved	[19]
Lopinavir	DMITQS0	Human immunodeficiency virus infection	1C62	Approved	[7]
Lovastatin	DM9OZWQ	Hypercholesterolaemia	5C80.0	Approved	[20]
Mesalazine	DMOL5IU	Ulcerative colitis	DD71	Approved	[21]
Methotrexate	DM2TEOL	leukaemia	2A60-2B33	Approved	[22]
Mycophenolate mofetil	DMPQAGE	Organ transplant rejection	NE84	Approved	[23]
Nafcillin	DMN9RPO	Arthritis	FA20	Approved	[7]
Nateglinide	DMLK2QH	Diabetic complication	5A2Y	Approved	[6]
Nilotinib	DM7HXWT	Chronic myelogenous leukaemia	2A20.0	Approved	[10]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[24]
Paclitaxel	DMLB81S	Breast cancer	2C60-2C65	Approved	[25]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[7]
Pitavastatin	DMJH792	Hyperlipidemia	5C80.Z	Approved	[26]
Pitavastatin calcium	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[27]
Pravastatin	DM6A0X7	Hypercholesterolaemia	5C80.0	Approved	[27]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[28]
Repaglinide	DM5SXUV	Diabetic complication	5A2Y	Approved	[29]
Rifampin	DMA8J1G	Tuberculosis	1B10-1B1Z	Approved	[30]
Rosuvastatin	DMMIQ7G	Hypercholesterolaemia	5C80.0	Approved	[31]
Saquinavir	DMG814N	Human immunodeficiency virus infection	1C62	Approved	[7]
Simeprevir	DMLUA9D	Chronic HCV-1 infection	1E51.1	Approved	[32]
Simvastatin	DM30SGU	Hypercholesterolaemia	5C80.0	Approved	[33]
Sirolimus	DMGW1ID	Multiple myeloma	2A83	Approved	[34]
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[10]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[10]
Technetium (99MTC) mebrofenin	DMUEWM3	Diagnostic imaging	N.A.	Approved	[29]
Temocapril	DM1A79H	High blood pressure	BA00	Approved	[7]
Torasemide	DMXKJ6C	Congestive heart failure	BD10	Approved	[35]
Ursodeoxycholic acid	DMCUT21	Primary biliary cirrhosis	DB96.1	Approved	[36]
Valsartan	DMREUQ6	Hypertension	BA00-BA04	Approved	[2]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[10]
Vemurafenib	DM62UG5	Melanoma	2C30	Approved	[10]
Primovist	DM37FKA	Lung cancer	2C25.0	Phase 4	[7]

12 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Atrasentan	DMM74PK	Diabetic nephropathy	GB61.Z	Phase 3	[7]
Benzylpenicillin	DMS9503	N. A.	N. A.	Phase 3	[7]
Karenitecin	DMCRGY4	Lung cancer	2C25.0	Phase 3	[7]
BQ-123	DM0MO8I	Pulmonary arterial hypertension	BB01.0	Phase 2	[7]
Cholyl lysyl fluorescein	DMALN2M	Hepatitis virus infection	1E50-1E51	Phase 2	[7]
Danoprevir	DM20MDU	Hepatitis C virus infection	1E51.1	Phase 2	[8]
Flavopiridol	DMKSUOI	Acute myeloid leukaemia	2A60	Phase 2	[7]
Gimatecan	DMSKMET	Breast cancer	2C60-2C65	Phase 2	[7]
LE-SN38	DMW50NF	Colorectal cancer	2B91.Z	Phase 2	[7]
Ym-758	DMU79X2	Angina pectoris	BA40	Phase 2	[7]
Sodium taurocholate	DM3GO0J	Type-2 diabetes	5A11	Phase 1/2	[2]
Taurocholic acid	DM2LZ8F	Type-2 diabetes	5A11	Phase 1/2	[19]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tr-14035	DMWD39E	Multiple sclerosis	8A40	Discontinued in Phase 1	[37]

8 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bilirubin	DMI0V4O	Discovery agent	N.A.	Investigative	[38]
Bromsulphthalein	DM9W2ZV	N. A.	N. A.	Investigative	[39]
CCK-8	DMN0J4W	N. A.	N. A.	Investigative	[7]
Dadle	DMRM0OW	Discovery agent	N.A.	Investigative	[7]
Fluo-3	DMLO9FU	Discovery agent	N.A.	Investigative	[40]
Glycocholic acid	DM0SXNM	Discovery agent	N.A.	Investigative	[7]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[7]
[3H]estradiol-17beta-glucuronide	DM3KJ45	Discovery agent	N.A.	Investigative	[41]

Molecular Expression Atlas (MEA) of This DTP

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Acute myelocytic leukaemia	2B33.1	Bone marrow	9.49E-02	5.87E-03	5.86E-02
Adrenocortical carcinoma	2D11.Z	Kidney	2.07E-01	3.07E-02	2.01E-01
Alopecia	ED70	Skin from scalp	2.75E-01	2.07E-02	9.26E-02
Alzheimer's disease	8A20	Entorhinal cortex	8.15E-01	6.20E-03	5.61E-02
Ankylosing spondylitis	FA92.0	Pheripheral blood	9.87E-01	1.11E-02	1.24E-01
Aortic stenosis	BB70	Calcified aortic valve	6.85E-01	-5.08E-02	-1.72E-01
Apnea	7A40	Hyperplastic tonsil	4.99E-01	-2.54E-04	-2.46E-03
Arthropathy	FA00-FA5Z	Peripheral blood	6.69E-01	4.88E-03	3.78E-02
Asthma	CA23	Nasal and bronchial airway	4.30E-05	7.91E-02	3.70E-01
Atopic dermatitis	EA80	Skin	3.30E-02	4.23E-02	2.51E-01
Autism	6A02	Whole blood	5.07E-01	-5.21E-02	-2.97E-01
Autoimmune uveitis	9A96	Peripheral monocyte	2.63E-01	-5.35E-02	-3.52E-01
Autosomal dominant monocytopenia	4B04	Whole blood	1.60E-02	-1.16E-01	-1.37E+00
Bacterial infection of gingival	1C1H	Gingival tissue	1.58E-03	4.02E-02	2.15E-01
Batten disease	5C56.1	Whole blood	7.27E-01	-9.38E-02	-1.09E+00
Behcet's disease	4A62	Peripheral blood	1.09E-01	-3.03E-02	-1.51E-01
Bipolar disorder	6A60-6A6Z	Prefrontal cortex	3.89E-01	-1.75E-02	-1.15E-01
Bladder cancer	2C94	Bladder tissue	1.23E-02	1.36E-02	1.01E-01
Breast cancer	2C60-2C6Z	Breast tissue	9.12E-01	9.67E-03	3.43E-02
Cardioembolic stroke	8B11.20	Whole blood	6.46E-01	-7.72E-02	-3.41E-01
Cervical cancer	2C77	Cervical tissue	1.35E-02	-9.49E-02	-4.27E-01
Childhood onset rheumatic disease	FA20.Z	Peripheral blood	9.37E-01	2.74E-02	1.51E-01
Chronic hepatitis C	1E51.1	Whole blood	4.29E-01	-1.04E-03	-1.20E-02
Chronic obstructive pulmonary disease	CA22	Lung tissue	2.41E-01	-2.63E-02	-8.50E-02
Chronic obstructive pulmonary disease	CA22	Small airway epithelium	5.54E-01	-1.65E-02	-1.24E-01
Chronic rhinosinusitis	CA0A	Sinus mucosa tissue	7.69E-01	1.88E-02	2.46E-01
Colon cancer	2B90	Colon tissue	3.12E-09	7.77E-02	3.84E-01
Coronary artery disease	BA80-BA8Z	Peripheral blood	3.17E-01	6.66E-02	4.62E-01
Diffuse large B-cell lymphoma	2A81	Tonsil tissue	2.93E-01	-1.09E-01	-3.82E-01
Endometriosis	GA10	Endometrium tissue	5.94E-01	-5.43E-03	-2.82E-02
Familial hypercholesterolemia	5C80.00	Peripheral blood	3.75E-01	6.66E-02	5.58E-01
Familial hypercholesterolemia	5C80.00	Whole blood	3.27E-01	-5.78E-02	-3.84E-01
Gastric cancer	2B72	Gastric tissue	9.20E-01	-1.59E-03	-9.27E-03
Glioblastopma	2A00.00	Nervous tissue	1.28E-02	-3.03E-02	-1.77E-01
Glioma	2A00.0Y-2A00.0Z	White matter tissue	1.27E-01	-1.70E-01	-5.42E-01
Head and neck cancer	2D42	Head and neck tissue	8.73E-01	1.50E-03	9.14E-03
HIV-associated neurocognitive impairment	8A2Y-8A2Z	White matter tissue	2.68E-01	-3.85E-02	-3.86E-01
Huntington's disease	8A01.10	Whole blood	2.23E-01	-6.79E-02	-4.89E-01
Idiopathic pulmonary fibrosis	CB03.4	Lung tissue	6.11E-01	-1.87E-01	-9.80E-01
Immunodeficiency	4A00-4A20	Peripheral blood	2.21E-01	-5.57E-02	-6.30E-01
Influenza	1.00E+30	Whole blood	1.58E-01	1.80E-01	1.63E+00
Interstitial cystitis	GC00.3	Bladder tissue	1.67E-02	7.40E-02	1.58E+00
Intracranial aneurysm	8B01.0	Intracranial artery	5.08E-01	-9.92E-02	-5.05E-01
Irritable bowel syndrome	DD91.0	Rectal colon tissue	7.76E-01	-8.58E-03	-4.87E-02
Ischemic stroke	8B11	Peripheral blood	8.66E-01	1.67E-02	1.04E-01
Juvenile idiopathic arthritis	FA24	Peripheral blood	3.41E-01	9.35E-02	3.49E-01
Lateral sclerosis	8B60.4	Cervical spinal cord	7.81E-01	-1.08E-01	-5.41E-01
Lateral sclerosis	8B60.4	Skin	5.23E-01	-1.00E-01	-3.26E-01
Liver cancer	2C12.0	Liver tissue	1.45E-26	-1.31E+00	-2.12E+00
Liver failure	DB99.7-DB99.8	Liver tissue	1.73E-03	-4.33E+00	-7.79E+00
Lung cancer	2C25	Lung tissue	2.80E-34	1.44E-01	9.71E-01
Lupus erythematosus	4A40	Whole blood	3.56E-04	5.83E-02	1.92E-01
Major depressive disorder	6A70-6A7Z	Whole blood	2.86E-01	9.09E-03	4.61E-02
Major depressive disorder	6A70-6A7Z	Hippocampus	8.47E-01	1.14E-02	8.20E-02
Melanoma	2C30	Skin	1.12E-01	-7.30E-02	-1.37E-01
Multiple myeloma	2A83.1	Bone marrow	1.50E-04	1.94E-01	2.06E+00
Multiple myeloma	2A83.1	Peripheral blood	6.86E-01	3.72E-02	2.86E-01
Multiple sclerosis	8A40	Plasmacytoid dendritic cells	3.23E-01	6.36E-02	5.84E-01
Myelodysplastic syndrome	2A36-2A3Z	Bone marrow	9.55E-01	1.20E-02	9.21E-02
Myelofibrosis	2A20.2	Whole blood	3.14E-04	9.49E-02	8.25E-01
Myocardial infarction	BA41-BA50	Peripheral blood	1.73E-02	1.07E-01	2.61E-01
Myopathy	8C70.6	Muscle tissue	4.62E-01	-8.97E-03	-6.28E-02
Neonatal sepsis	KA60	Whole blood	2.70E-01	-2.71E-02	-1.46E-01
Neuroectodermal tumour	2A00.11	Brain stem tissue	6.37E-01	-1.96E-03	-1.14E-02
Non-alcoholic fatty liver disease	DB92	Liver tissue	2.00E-02	7.38E-01	9.90E-01
Obesity related type 2 diabetes	5A11	Omental adipose tissue	5.57E-01	1.53E-02	1.76E-01
Olive pollen allergy	CA08.00	Peripheral blood	1.25E-01	-8.96E-02	-5.03E-01
Oral cancer	2B6E	Oral tissue	2.47E-04	1.32E-01	7.89E-01
Osteoarthritis	FA00-FA0Z	Synovial tissue	9.30E-01	7.68E-02	3.82E-01
Osteoporosis	FB83.1	Bone marrow	7.68E-02	1.80E-01	1.25E+00
Ovarian cancer	2C73	Ovarian tissue	5.40E-01	-3.16E-02	-1.22E-01
Pancreatic cancer	2C10	Pancreas	9.07E-02	-9.94E-02	-5.12E-01
Parkinson's disease	8A00.0	Substantia nigra tissue	8.03E-01	8.37E-02	4.07E-01
Pediatric respiratory syncytial virus infection	CA40.11	Peripheral blood	2.07E-01	5.26E-02	4.81E-01
Pituitary cancer	2D12	Pituitary tissue	1.88E-02	1.77E-01	9.29E-01
Pituitary gonadotrope tumour	2D12	Pituitary tissue	6.46E-02	2.08E-01	1.09E+00
Polycystic ovary syndrome	5A80.1	Vastus lateralis muscle	3.33E-01	-5.25E-03	-4.09E-02
Polycythemia vera	2A20.4	Whole blood	3.85E-09	1.32E-01	1.12E+00
Pompe disease	5C51.3	Biceps muscle	1.38E-01	-1.46E-01	-1.22E+00
Preterm birth	KA21.4Z	Myometrium	7.18E-01	-5.08E-02	-4.53E-01
Prostate cancer	2C82	Prostate	7.59E-01	-3.08E-02	-1.64E-01
Psoriasis	EA90	Skin	3.65E-04	-1.54E-01	-7.81E-01
Rectal cancer	2B92	Rectal colon tissue	2.48E-01	-8.99E-02	-4.81E-01
Renal cancer	2C90-2C91	Kidney	6.76E-03	8.67E-02	6.17E-01
Retinoblastoma	2D02.2	Uvea	3.26E-02	1.34E-01	1.81E+00
Rheumatoid arthritis	FA20	Synovial tissue	5.71E-01	-1.33E-02	-6.44E-02
Rhinovirus infection	CA42.1	Nasal epithelium tissue	3.13E-01	3.50E-03	3.41E-02
Schizophrenia	6A20	Prefrontal cortex	9.01E-01	3.70E-03	2.13E-02
Schizophrenia	6A20	Superior temporal cortex	9.70E-01	2.57E-03	2.16E-02
Scleroderma	4A42.Z	Whole blood	1.26E-03	2.42E-01	1.68E+00
Seizure	8A60-8A6Z	Whole blood	4.28E-01	-5.35E-02	-3.18E-01
Sensitive skin	EK0Z	Skin	4.49E-01	-1.07E-01	-8.21E-01
Sepsis with septic shock	1G41	Whole blood	2.45E-01	3.59E-02	1.70E-01
Shwachman-Diamond syndrome	3A70.0	Bone marrow	5.08E-01	-2.87E-02	-2.90E-01
Sickle cell disease	3A51.0-3A51.3	Peripheral blood	1.90E-01	8.99E-03	9.09E-02
Simpson golabi behmel syndrome	LD2C	Adipose tissue	9.30E-01	6.08E-02	3.23E-01
Sjogren's syndrome	4A43.2	Salivary gland tissue	1.00E-01	-3.29E-01	-1.92E+00
Skin cancer	2C30-2C3Z	Skin	2.65E-04	5.83E-02	1.94E-01
Thrombocythemia	3B63	Whole blood	2.66E-02	2.54E-02	2.28E-01
Thrombocytopenia	3B64	Whole blood	9.08E-02	1.19E-01	5.19E-01
Thyroid cancer	2D10	Thyroid	5.98E-03	9.85E-03	5.46E-02
Tibial muscular dystrophy	8C75	Muscle tissue	1.37E-01	-9.96E-02	-4.51E-01
Tuberous sclerosis complex	LD2D.2	Perituberal tissue	2.24E-01	5.34E-02	6.68E-01
Type 2 diabetes	5A11	Liver tissue	2.81E-01	3.67E-02	2.82E-01
Ureter cancer	2C92	Urothelium	9.93E-01	-8.70E-02	-4.54E-01
Uterine cancer	2C78	Endometrium tissue	1.12E-01	8.17E-03	5.03E-02
Vitiligo	ED63.0	Skin	5.69E-01	-2.82E-02	-1.27E-01

Drug Affinity of This DTP Assessed by Cell Line

Approved Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
Atorvastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 0.77 microM	[42]
Atorvastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 12.4 microM	[43]
Atorvastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 18.9 microM	[44]
Bosentan	Approved	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 44 microM	[5]
Cilostazol	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 17.7 microM	[9]
Fluvastatin	Approved	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 1.4 microM	[45]
Fluvastatin	Approved	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 3.5 microM	[45]
Fluvastatin	Approved	Oocytes-OATP1B1	Km = 31.1 microM	[27]
Levothyroxine	Approved	Oocytes-OATP1B1	Km = 3 microM	[19]
Liothyronine	Approved	Oocytes-OATP1B1	Km = 2.7 microM	[19]
Mesalazine	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 55.1 microM	[21]
Olmesartan medoxomil	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 12.8 microM	[46]
Olmesartan medoxomil	Approved	Oocytes-OATP1B1	Km = 42.6 microM	[24]
Pitavastatin calcium	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 3 microM	[47]
Pitavastatin calcium	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 4.8 microM	[48]
Pitavastatin calcium	Approved	Oocytes-OATP1B1	Km = 3.6 microM	[49]
Pitavastatin calcium	Approved	Oocytes-OATP1B1	Km = 6.7 microM	[27]
Pravastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 33.7 microM	[20]
Pravastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 85.7 microM	[43]
Pravastatin	Approved	Oocytes-OATP1B1	Km = 57.5 microM	[27]
Rifampin	Approved	Human cervical cancer cell line (Hela)-OATP1B1	Km = 1.5 microM	[30]
Rifampin	Approved	Oocytes-OATP1B1	Km = 13 microM	[50]
Rosuvastatin	Approved	Human cervical cancer cell line (Hela)-OATP1B1	Km = 4 microM	[51]
Rosuvastatin	Approved	Human cervical cancer cell line (Hela)-OATP1B1	Km = 7.3 microM	[51]
Rosuvastatin	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 0.8 microM	[31]
Rosuvastatin	Approved	Oocytes-OATP1B1	Km = 8.5 microM	[52]
Valsartan	Approved	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 17.8 microM	[53]
Valsartan	Approved	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 1.39 microM	[54]

Clinical Trial Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
Taurocholic acid	Phase 1/2	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 33.8 microM	[20]
Taurocholic acid	Phase 1/2	Oocytes-OATP1B1	Km = 13.6 microM	[19]

Investigative Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
Bilirubin	Investigative	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 0.1 microM	[55]
Bilirubin	Investigative	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 0.28 microM	[55]
Bilirubin	Investigative	Oocytes-OATP1B1	Km = 0.0076 microM	[38]
Bromsulphthalein	Investigative	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 0.14 microM	[55]
Bromsulphthalein	Investigative	Oocytes-OATP1B1	Km = 0.3 microM	[39]
[3H]estradiol-17beta-glucuronide	Investigative	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 5.4 microM	[40]
[3H]estradiol-17beta-glucuronide	Investigative	Chinese hamster ovary (CHO) cells-OATP1B1	Km = 5.9 microM	[41]
[3H]estradiol-17beta-glucuronide	Investigative	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 2.5 microM	[56]
[3H]estradiol-17beta-glucuronide	Investigative	Human embryonic kidney cells (HEK293)-OATP1B1	Km = 8.29 microM	[47]

The Drug Therapeutic Target (DTT) Role of This DTP

• DTP DTT Name: Liver organic anion transporter 1 (SLCO1B1) DTT Info
• DTP DTT Type: Literature-reported

2 Investigative Drug(s) Targeting This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
[3H]estradiol-17beta-glucuronide	DM3KJ45	Discovery agent	N.A.	Investigative	[1]
[3H]estrone-3-sulphate	DMGPF0N	Discovery agent	N.A.	Investigative	[1]

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