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ChEMBL ligand: CHEMBL189123 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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B1 receptor/Bradykinin B1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663] | ||||||||
ChEMBL | Binding affinity to human BK1 receptor Q295 mutant | B | 9.05 | pKi | 0.89 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929] |
ChEMBL | Binding affinity to human BK1 receptor D291 mutant | B | 10.31 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929] |
ChEMBL | Binding affinity to human BK1 receptor N298 mutant | B | 10.42 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929] |
ChEMBL | Displacement of [3H]Lys0-des-Arg9-BK at human bradykinin B1 receptor expressed in HEK293 cells | B | 10.47 | pKi | 0.03 | nM | Ki | J Med Chem (2010) 53: 5383-5399 [PMID:20369879] |
ChEMBL | Binding affinity to human bradykinin B1 receptor | B | 10.47 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3095-3099 [PMID:22483585] |
ChEMBL | Binding affinity to human BK1 receptor | B | 10.47 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929] |
ChEMBL | Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D-/aequorin cells by rapid filtration technique | B | 10.47 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4477-4481 [PMID:18674903] |
GtoPdb | - | - | 10.5 | pKi | - | - | - | J Am Chem Soc (2003) 125: 7516-7 [PMID:12812482] |
ChEMBL | Binding affinity to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay | B | 10.52 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6045-6048 [PMID:15546726] |
ChEMBL | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells | F | 9.74 | pIC50 | 0.18 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4477-4481 [PMID:18674903] |
ChEMBL | Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation | F | 9.74 | pIC50 | 0.18 | nM | IC50 | J Med Chem (2010) 53: 5383-5399 [PMID:20369879] |
Bradykinin B1 receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4724] [UniProtKB: Q9BDQ5] | ||||||||
ChEMBL | Antagonist activity at dog bradykinin B1 receptor | F | 7.79 | pIC50 | 16.3 | nM | IC50 | J Med Chem (2010) 53: 5383-5399 [PMID:20369879] |
Bradykinin B1 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4087] [UniProtKB: P48748] | ||||||||
ChEMBL | Inhibition of rabbit bradykinin B1 receptor | B | 9.59 | pIC50 | 0.26 | nM | IC50 | J Med Chem (2010) 53: 5383-5399 [PMID:20369879] |
B1 receptor/Bradykinin B1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | J Am Chem Soc (2003) 125: 7516-7 [PMID:12812482] |
ChEMBL | Inhibition of rat bradykinin B1 receptor | B | 6.79 | pIC50 | 163.5 | nM | IC50 | J Med Chem (2010) 53: 5383-5399 [PMID:20369879] |
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411] | ||||||||
ChEMBL | Binding affinity to human Bradykinin receptor B2 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6045-6048 [PMID:15546726] |
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]