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 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]
