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/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 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 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]
