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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 |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]