timapiprant [Ligand Id: 9277] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL560993 (CHF-6532, Oc000459, OC-000459, OC000459, Oc-459, OC459, Odc-9101, Timapiprant) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943] | ||||||||
| ChEMBL | Inhibition of rat aldose reductase | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
| ChEMBL | Antagonistic activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced calcium mobilization after 60 mins by Fluo-3 based fluorescence assay | F | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| GtoPdb | Displacement of [3H]PGD2 from human recombinant DP2 | - | 7.89 | pKi | 13 | nM | Ki | J Pharmacol Exp Ther (2012) 340: 473-82 [PMID:22106101] |
| ChEMBL | Antagonist activity at CRTh2 receptor (unknown origin) overexpressed in CHOK1 cell membranes assessed as inhibition of [35S]-GTPgammaS binding preincubated for 1 hr followed by 50 nM PGD2 and 0.1 nM [35S]-GTPgammaS addition measured after 2 hrs by liquid scintillation counting analysis | F | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3349-3353 [PMID:23601708] |
| ChEMBL | Inhibition of CRTH2 in human whole blood | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| ChEMBL | Displacement of [3H]PGD2 from human prostaglandin D2 receptor in presence of human serum albumin | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
| ChEMBL | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced antiapoptotic activity | F | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| ChEMBL | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced chemotaxis | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| ChEMBL | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced IL13 production | F | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| ChEMBL | Displacement of [3H]PGD2 from human prostaglandin D2 receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
| ChEMBL | Antagonist activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced shape change | F | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
| DP2 receptor in Rat [GtoPdb: 339] [UniProtKB: Q6XKD3] | ||||||||
| GtoPdb | Displacement of [3H]PGD2 from rat recombinant DP2 | - | 8.52 | pKi | 3 | nM | Ki | J Pharmacol Exp Ther (2012) 340: 473-82 [PMID:22106101] |
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Displacement of [3H]PGD2 from prostaglandin D1 receptor in human platelet membrane | B | 5.14 | pIC50 | 7300 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Displacement of [3H]iloprost from human prostacyclin receptor expressed in human 293 cell membrane | B | 4.24 | pIC50 | 57900 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
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]
