PMX53 [Ligand Id: 579] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL41547 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| C5a1 receptor/C5a anaphylatoxin chemotactic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2373] [GtoPdb: 32] [UniProtKB: P21730] | ||||||||
| ChEMBL | Antagonist activity against the C5a receptor | F | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2002) 45: 1543-1558 [PMID:11931608] |
| ChEMBL | Inhibition of C5a binding to human C5aR expressed in HEK293 cells | B | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| ChEMBL | Antagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase release | F | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| ChEMBL | Antagonist activity at C5aR1 in human PMN | F | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2018) 61: 3253-3276 [PMID:28977749] |
| ChEMBL | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | F | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| ChEMBL | Antagonist activity at C5aR1 in HMDM | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 3253-3276 [PMID:28977749] |
| GtoPdb | - | - | 7.7 | pIC50 | 21 | nM | IC50 |
Inflammation (2001) 25: 171-7 [PMID:11403208]; Mol Pharmacol (2004) 65: 868-79 [PMID:15044616]; BMC Biophys (2014) 7: 5 [PMID:25170421]; J Pharmacol Exp Ther (2014) 351: 344-51 [PMID:25150279] |
| ChEMBL | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | B | 7.8 | pIC50 | 15.85 | nM | IC50 | J Med Chem (2010) 53: 4938-4948 [PMID:20527893] |
| ChEMBL | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2010) 53: 4938-4948 [PMID:20527893] |
| MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] | ||||||||
| ChEMBL | Binding affinity to MC4 receptor | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | Binding affinity to NK2 receptor | B | 7.06 | pIC50 | 87 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Binding affinity to ORL1 receptor | B | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Binding affinity to V1a receptor | B | 6.13 | pIC50 | 740 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5088-5092 [PMID:16876401] |
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]
