PF-03654746 [Ligand Id: 9058] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2151197 (Pf-03654746, PF 03654746) |
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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] | ||||||||
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 8.64 | pKi | 2.29 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| GtoPdb | - | - | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2011) 54: 7602-20 [PMID:21928839] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
| GtoPdb | - | - | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2011) 54: 7602-20 [PMID:21928839] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 7.43 | pKi | 37.15 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.05 | pKi | 8.91 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
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]
