A-317920 [Ligand Id: 1216] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL361355 (A-317920) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456] |
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | B | 7.03 | pKi | 93.33 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | B | 7.03 | pKi | 93 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Binding affinity to rat cortical histamine H3 receptor | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456] |
| H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456] |
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]
