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: CHEMBL2386081 (ACT-129968, KYTH-105, Setipiprant) |
---|
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!
|
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 |
---|---|---|---|---|---|---|---|---|
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Antagonist activity at ovine COX-1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
ChEMBL | Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis in presence of human serum albumin | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
ChEMBL | Antagonist activity at CRTH2 receptor in human eosinophils assessed as inhibition of PGD2-induced cell shape change incubated for 1 hr prior to PGD2 induction measured after 5 mins by FACS flow cytometric analysis in presence of human plasma | B | 6.63 | pIC50 | 235 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
ChEMBL | Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2/forskolin-induced intracellular cAMP production after 20 mins by ELISA | F | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
ChEMBL | Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2-induced calcium flux after 5 mins by FLIPR assay | F | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2013) 56: 4899-911 [PMID:23721423] |
ChEMBL | Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
ChEMBL | Displacement of [3H]PGD2 from recombinant human prostanoid DP1 receptor expressed in CHO cells after 90 mins by scintillation counting analysis | B | 5.89 | pIC50 | 1290 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
ChEMBL | Antagonist activity at human prostanoid EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay | F | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
ChEMBL | Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
ChEMBL | Antagonist activity at human prostanoid EP3 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay | F | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
ChEMBL | Inhibition of beta-arrestin binding to recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
ChEMBL | Displacement of [3H]PGE2 from recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
ChEMBL | Antagonist activity at human prostanoid TP2 receptor expressed in HEK293 cells assessed as inhibition of calcium flux after 30 to 40 mins by FLIPR assay | F | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2013) 56: 4899-4911 [PMID:23721423] |
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]