L838417 [Ligand Id: 4241] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL373250 (L-838417) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
| ChEMBL | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Displacement of [3H]-flumazenil from human GABAA alpha1beta3gamma2 expressed in Ltk cells | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869] | ||||||||
| ChEMBL | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Displacement of [3H]-flumazenil from human GABAA alpha3beta3gamma2 expressed in Ltk cells | B | 9.17 | pKi | 0.67 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Displacement of [3H]-flumazenil from human GABAA alpha5beta3gamma2 expressed in Ltk cells | B | 8.65 | pKi | 2.25 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869] | ||||||||
| ChEMBL | Positive allosteric modulation of GABAA alpha2 (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
| ChEMBL | Positive allosteric modulation of GABAA alpha3 (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
| ChEMBL | Positive allosteric modulation of GABAA alpha5 (unknown origin) | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
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]
