A-304121 [Ligand Id: 1258] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL302196 (A-304121) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Binding affinity towards Histamine H1 receptor of human membranes. | B | 4.16 | pKi | 69183.1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2035-2037 [PMID:12113836] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | Binding affinity towards Histamine H2 receptor from human membranes | B | 4.15 | pKi | 70794.58 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2035-2037 [PMID:12113836] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 6.1 | pKi | 794.33 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| GtoPdb | - | - | 6.1 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456] |
| ChEMBL | Binding affinity for human histamine H3 receptor on human colon cells | B | 6.12 | pKi | 760 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 673-676 [PMID:14741266] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | B | 6.12 | pKi | 760 | 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 | 6.12 | pKi | 758.58 | 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 | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Binding affinity to rat cortical histamine H3 receptor | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Binding affinity towards Histamine H3 receptor of rat cortical membranes. | B | 8.9 | pKi | 1.26 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2035-2037 [PMID:12113836] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | Tested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assay | F | 6.98 | pKd | 104.71 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 2035-2037 [PMID:12113836] |
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]
