MK-2894 [Ligand Id: 4041] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL597997 (MK-2894) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 human DP2 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 4.68 | pKi | >21000 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Displacement of [3H]PGD2 from human DP1 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.41 | pKi | >3900 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.25 | pKi | >5600 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP1 receptor/Prostanoid EP1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5068] [GtoPdb: 340] [UniProtKB: P70597] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from rat EP1 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 4.54 | pKi | >29000 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.23 | pKi | 5900 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP2 receptor/Prostanoid EP2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.14 | pKi | 7200 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.1 | pKi | >7900 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP3 receptor/Prostanoid EP3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5674] [GtoPdb: 342] [UniProtKB: P34980] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting in presence of 10% human serum | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| GtoPdb | - | - | 9.25 | pKi | 0.56 | nM | Ki |
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]; J Med Chem (2010) 53: 2227-38 [PMID:20163116]; J Pharmacol Exp Ther (2008) 325: 425-34 [PMID:18287210] |
| ChEMBL | Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| ChEMBL | Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding. | B | 9.3 | pKi | 0.5 | nM | Ki | US-8969394-B2. Thiophenecarboxamide derivatives as EP4 receptor ligands (2015) |
| ChEMBL | Activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release | F | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| ChEMBL | Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum | F | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| ChEMBL | Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | F | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| ChEMBL | Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| EP4 receptor/Prostanoid EP4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from rat EP4 receptor expressed in HEK293-EBNA cells by scintillation counting | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088] | ||||||||
| ChEMBL | Displacement of [3H]PGF2alpha from human FP receptor expressed in HEK293-EBNA cells by scintillation counting | B | 4.62 | pKi | >24000 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Displacement of [3H]iloprost from human IP receptor expressed in HEK293-EBNA cells by scintillation counting | B | 4.66 | pKi | >22000 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Displacement of [3H]SQ29548 from human TP receptor expressed in HEK293-EBNA cells by scintillation counting | B | 5.17 | pKi | >6800 | nM | Ki | J Med Chem (2010) 53: 2227-2238 [PMID:20163116] |
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]
