Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTLA931)

• DTT Name: Neuronal acetylcholine receptor alpha-7 (CHRNA7)
• Synonyms: Nicotinic acetylcholine receptor subunit alpha 7; Nicotinic acetylcholine receptor alpha7; CHRNA7; Alpha7 nicotinic receptor; Alpha7 nAChR; Alpha-7 nAChR; Alpha(7) nicotinic receptor
• Gene Name: CHRNA7
• DTT Type: Successful target; [1]
• Related Disease:
  Corneal disease [ICD-11: 9A76-9A78]
  Schizophrenia [ICD-11: 6A20]
• BioChemical Class: Neurotransmitter receptor
• UniProt ID: ACHA7_HUMAN
• TTD ID: T34429
• Sequence:
  MRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLL
  QIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADE
  RFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDL
  QMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIP
  CVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFAST
  MIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHK
  QRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHL
  LHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTI
  ICTIGILMSAPNFVEAVSKDFA
• Function: After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Cholinergic synapse (hsa04725)
  Nicotine addiction (hsa05033)
  Chemical carcinogenesis (hsa05204)
• Reactome Pathway: Highly calcium permeable postsynaptic nicotinic acetylcholine receptors (R-HSA-629594)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ALCURONIUM	DM2U4XQ	Anaesthesia	9A78.6	Approved	[2]
Ziprasidone	DMM58JY	Schizophrenia	6A20	Approved	[1]

13 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[3]
CYTISINE	DMUF0BJ	Tobacco dependence	6C4A.2	Phase 3	[4]
EVP-6124	DMLQO7F	Alzheimer disease	8A20	Phase 3	[5]
ABT-126	DM2OS51	Alzheimer disease	8A20	Phase 2	[6]
AQW-051	DMD2RFO	Alzheimer disease	8A20	Phase 2	[7]
GTS-21	DMEN5KA	Parkinson disease	8A00.0	Phase 2	[8], [9]
JNJ-39393406	DMUOEKM	Depression	6A70-6A7Z	Phase 2	[10]
MEM-3454	DMPNDYU	Schizophrenia	6A20	Phase 2	[1]
TC-6987	DMNFP21	Asthma	CA23	Phase 2	[11]
AVL-3288	DMGAKR9	Cognitive impairment	6D71	Phase 1	[12]
BMS-933043	DMG3J6C	Psychiatric disorder	6E8Z	Phase 1	[13]
BNC375	DMI4UY3	Cognitive impairment	6D71	Phase 1	[14]
R4996	DMSKHIC	Neurological disorder	6B60	Phase 1	[3]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD-9684	DMHA5ME	Thrombosis	DB61-GB90	Discontinued in Phase 2	[15]
AZD0328	DM4B7CM	Alzheimer disease	8A20	Discontinued in Phase 2	[16]
ABT-107	DMPCYV6	Attention deficit hyperactivity disorder	6A05.Z	Discontinued in Phase 1	[17]
PNU-282987	DMGDC36	Schizophrenia	6A20	Terminated	[1]

2 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PHA-568487	DMM149N	Cognitive impairment	6D71	Preclinical	[18]
RMG-40083	DMJGQD2	Schizophrenia	6A20	Preclinical	[1]

24 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3,8-dibromoboldine	DM23CEI	Discovery agent	N.A.	Investigative	[19]
3-bromoboldine	DMPF7O2	Discovery agent	N.A.	Investigative	[19]
4BP-TQS	DMS0JVE	Discovery agent	N.A.	Investigative	[20]
A-582941	DM7R8DJ	Discovery agent	N.A.	Investigative	[21]
A-867744	DM96F8U	Discovery agent	N.A.	Investigative	[22]
AZD-6319	DMD4YO9	Alzheimer disease	8A20	Investigative	[23]
Barbituric acid derivative	DM2I19P	Discovery agent	N.A.	Investigative	[24]
CP-810123	DMXDG13	Discovery agent	N.A.	Investigative	[25]
EVP-4473	DMHMFKE	Alzheimer disease	8A20	Investigative	[23]
GCCSHPACAGNNQHIC*	DM4BZEC	Discovery agent	N.A.	Investigative	[26]
GCCSNPVCHLEHSNLC*	DMJ0ICN	Discovery agent	N.A.	Investigative	[26]
JN-711	DMFU76I	Central nervous system disease	8A04-8D87	Investigative	[23]
JNJ-1930942	DMKH9O7	Cognitive impairment	6D71	Investigative	[23]
LY2087101	DMIS82X	Discovery agent	N.A.	Investigative	[27]
NS1738	DM2S5ZF	Discovery agent	N.A.	Investigative	[28]
PH-709829	DM5GY6Z	Discovery agent	N.A.	Investigative	[29]
PheTQS	DMWMBP3	Central nervous system disease	8A04-8D87	Investigative	[23]
PNU-120596	DMYBQM7	Discovery agent	N.A.	Investigative	[30]
PSAB-OFP	DM38JMK	Discovery agent	N.A.	Investigative	[31]
TOXIFERINE	DMJHTQK	Discovery agent	N.A.	Investigative	[2]
[125I]epibatidine	DMZWQH3	Discovery agent	N.A.	Investigative	[23]
[3H]A-585539	DMSDY2Z	Discovery agent	N.A.	Investigative	[32]
[3H]AZ11637326	DMPVG5Y	Discovery agent	N.A.	Investigative	[33]
[3H]methyllycaconitine	DMYWGCS	Discovery agent	N.A.	Investigative	[23], [34], [35]

References

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