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 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]
