A-85380 [Ligand Id: 5460] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL59986 (A-85380) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907588] [GtoPdb: 462, 475, 471, 476] [UniProtKB: P02708, P07510, P11230, Q07001] | ||||||||
| ChEMBL | Binding affinity to muscle type alpha1beta1gammadelta-nAChR | B | 6.5 | pKi | 314 | nM | Ki | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| ChEMBL | Antagonist activity at human alpha1beta1gammadelta nAChR | B | 6.5 | pKi | 314 | nM | Ki | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
| Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [125 I]alpha-bungarotoxin (alpha-BgT) from torpedo alpha1-beta1-gamma1 electroplax | B | 6.5 | pKi | 314 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P04757, P09483, P12389, P12390, P12391, P12392, P20420, P43143, P43144, Q05941, Q9JLB5] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [3H]-cytisine binding from high-affinity Nicotinic acetylcholine receptor in rat brain (principally the alpha4-beta2 nAChR subtype) | B | 9.28 | pKi | 0.52 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand | B | 9.66 | pKi | 0.22 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain. | B | 10.28 | pKi | 0.05 | nM | Ki | J Med Chem (1996) 39: 817-825 [PMID:8632405] |
| ChEMBL | Binding affinity towards nicotinic acetylcholine receptor using [3H]nicotine as radioligand in rat brain homogenates | B | 10.3 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1989-1992 [PMID:12113825] |
| nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907592] [GtoPdb: 463, 472] [UniProtKB: P12389, P12390] | ||||||||
| ChEMBL | Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 10.13 | pKi | 0.07 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907587] [GtoPdb: 464, 472] [UniProtKB: P04757, P12390] | ||||||||
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.62 | pKi | 0.24 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) | B | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907593] [GtoPdb: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 7.14 | pKi | 72 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| ChEMBL | Agonist activity at alpha4beta2 nAChR (unknown origin) | B | 10.28 | pKi | 0.05 | nM | Ki | J Med Chem (2014) 57: 3966-3983 [PMID:24814197] |
| ChEMBL | Binding affinity against human Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (1999) 42: 2251-2259 [PMID:10377231] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Binding affinity to alpha4beta2 nAChR in human brain | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| ChEMBL | Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin) | B | 10.4 | pKi | 0.04 | nM | Ki | Med Chem Res (2005) 14: 241-259 |
| ChEMBL | Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in HEK293 cells | B | 8.82 | pIC50 | 1.51 | nM | IC50 | J Med Chem (2009) 52: 2311-2316 [PMID:19301898] |
| ChEMBL | Agonist activity at human alpha4beta2 nAChR expressed in HEK293 cells assessed as intracellular calcium level by FLIPR assay | F | 6.15 | pEC50 | 707.95 | nM | EC50 | J Med Chem (2009) 52: 2311-2316 [PMID:19301898] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2 | B | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Agonist activity at human alpha4beta2 nAChR | F | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| ChEMBL | Agonist activity at human alpha4beta2 nAChR | B | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.85 | pKi | 0.14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 in rat brain using [3H]-cytisine as radioligand | B | 10.28 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2797-2802 [PMID:9873625] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nACHR | B | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (2012) 55: 812-823 [PMID:22148173] |
| ChEMBL | Binding affinity to alpha4beta2 nAChR in rat brain | B | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| ChEMBL | Binding affinity for alpha4 beta-2 nAChR using [3H]epibatidine in rat brain | B | 10.77 | pKi | 0.02 | nM | Ki | J Med Chem (1998) 41: 3690-3698 [PMID:9733494] |
| ChEMBL | In vitro binding affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membrane using [3H]cytisine as radioligand | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2000) 43: 2217-2226 [PMID:10841800] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907595] [GtoPdb: 465, 474] [UniProtKB: P09483, P12392] | ||||||||
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 8.15 | pKi | 7.1 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [125I]alpha-bungarotoxin (alpha-BgT) from K28 cells expressing human Nicotinic acetylcholine receptor alpha7 | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Binding affinity against human Nicotinic acetylcholine receptor alpha-7 was determined | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (1999) 42: 2251-2259 [PMID:10377231] |
| ChEMBL | Binding affinity to human alpha7 nAChR in human brain | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| ChEMBL | Agonist activity at alpha7 nAChR (unknown origin) | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (2014) 57: 3966-3983 [PMID:24814197] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha7 | B | 5.05 | pEC50 | 8900 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Compound was evaluated for functional activation from channel currents at human Nicotinic acetylcholine receptor alpha-7 expressed in oocytes. | F | 5.05 | pEC50 | 8900 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Agonist activity at human alpha7 nAChR | F | 5.05 | pEC50 | 8900 | nM | EC50 | J Med Chem (2012) 55: 9998-10009 [PMID:23092294] |
| nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor subunit alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3068] [GtoPdb: 464] [UniProtKB: P32297] | ||||||||
| ChEMBL | Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype | F | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
