tebanicline [Ligand Id: 3989] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL430497 (Tebanicline) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 5 | pKi | 10000 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Compound was evaluated for its ability to displace [125 I]alpha-bungarotoxin (alpha-BgT) from torpedo alpha1-beta1-gamma1 electroplax | B | 5.47 | pKi | 3400 | 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 | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| 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 | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| GtoPdb | - | - | 10.43 | pKi | 0.04 | nM | Ki | J Pharmacol Exp Ther (1998) 285: 777-86 [PMID:9580626] |
| 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 | Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | F | 6.72 | pEC50 | 190 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| 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 | Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.26 | pKi | 0.06 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]cytisine from K177 cells expressing human Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.47 | pKi | 0.03 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| 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 | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane | B | 10.32 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 in rat brain using [3H]-cytisine as radioligand | B | 10.4 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2797-2802 [PMID:9873625] |
| GtoPdb | - | - | 10.43 | pKi | 0.04 | nM | Ki | J Pharmacol Exp Ther (1998) 285: 777-86 [PMID:9580626] |
| 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 | 5.57 | pKi | 2670 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Compound was evaluated for its ability to displace [125I]alpha-bungarotoxin (alpha-BgT) from K28 cells expressing human Nicotinic acetylcholine receptor alpha7 | B | 5.69 | pKi | 2060 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Compound was evaluated for functional activation from channel currents at human Nicotinic acetylcholine receptor alpha-7 expressed in oocytes. | F | 4.25 | pEC50 | 56000 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Compound was evaluated for functional activation from channel currents at human Nicotinic acetylcholine receptor alpha-7 expressed in oocytes. | B | 4.68 | pEC50 | 21000 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| 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 | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype | F | 6.89 | pEC50 | 130 | 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]
