pyrazolone, 1 [Ligand Id: 5831] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL379761 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462] | ||||||||
| ChEMBL | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay | B | 7.29 | pEC50 | 51.29 | nM | EC50 | J Med Chem (2019) 62: 5242-5248 [PMID:31038950] |
| ChEMBL | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay | F | 7.49 | pEC50 | 32.36 | nM | EC50 | J Med Chem (2019) 62: 5242-5248 [PMID:31038950] |
| FPR1 in Mouse [GtoPdb: 222] [UniProtKB: P33766] | ||||||||
| GtoPdb | - | - | 8.7 | pEC50 | - | - | - | Mol Pharmacol (2013) 83: 389-98 [PMID:23160941] |
| FPR2/ALX/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090] | ||||||||
| ChEMBL | Biased agonist activity at human FPR2 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay | F | 7.02 | pEC50 | 95.5 | nM | EC50 | J Med Chem (2019) 62: 5242-5248 [PMID:31038950] |
| ChEMBL | Activity at human FPRL1-mediated calcium mobilization in CHO cells | F | 7.36 | pEC50 | 44 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3713-3718 [PMID:16697190] |
| ChEMBL | Agonist activity at human recombinant FPRL1 expressed in CHO cells assessed as calcium flux by aequorin based bioluminescence assay | F | 7.36 | pEC50 | 44 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6633-6637 [PMID:17920884] |
| ChEMBL | Biased agonist activity at human FPR2 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay | B | 7.39 | pEC50 | 40.74 | nM | EC50 | J Med Chem (2019) 62: 5242-5248 [PMID:31038950] |
| GtoPdb | - | - | 7.4 | pEC50 | - | - | - | Bioorg Med Chem Lett (2006) 16: 3713-8 [PMID:16697190] |
| FPR2/ALX in Mouse [GtoPdb: 223] [UniProtKB: O88536] | ||||||||
| GtoPdb | - | - | 6.92 | pEC50 | - | - | - | Mol Pharmacol (2013) 83: 389-98 [PMID:23160941] |
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]
