timapiprant [Ligand Id: 9277] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL560993 (CHF-6532, Oc000459, OC-000459, OC000459, Oc-459, OC459, Odc-9101, Timapiprant) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
