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ChEMBL ligand: CHEMBL361812 (Baynas, BAY U 3405, BAY-U-3405, EN 137774, EN-137774, Ramatroban) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
ChEMBL | Inhibitory concentration for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium | F | 6.47 | pKi | 340 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1749-1753 [PMID:15745833] |
ChEMBL | Inhibitory activity for binding of PGD-2 to CRTH-2 in hCRTH-2 binding assay using HEK293 cell membranes | F | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1749-1753 [PMID:15745833] |
ChEMBL | Inhibitory activity for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium | F | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1749-1753 [PMID:15745833] |
ChEMBL | Binding affinity to human recombinant CRTH2 receptor by cell based radioligand equilibrium competition assay | B | 6.86 | pKi | 137 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 288-293 [PMID:21106375] |
ChEMBL | Displacement of [3H]PGD2 from human CRTh2 receptor expressed in CHO cells | B | 7.14 | pKi | 73 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4794-4798 [PMID:19592244] |
GtoPdb | - | - | 7.4 | pKi | - | - | - | Eur J Pharmacol (2005) 524: 30-7 [PMID:16256979] |
ChEMBL | Inhibition of [3H]PGD-2 binding to human chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Displacement of [3H]PGD2 from human prostaglandin D2 receptor in presence of human serum albumin | B | 6.12 | pIC50 | 754 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
ChEMBL | Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as inhibition of PGD2-mediated Ca2+ flux | F | 6.34 | pIC50 | 461 | nM | IC50 | J Med Chem (2011) 54: 1779-1788 [PMID:21355602] |
ChEMBL | Displacement of [3H]PGD2 from human prostaglandin D2 receptor | B | 6.51 | pIC50 | 311 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
ChEMBL | Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as effect on cAMP accumulation | F | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4794-4798 [PMID:19592244] |
ChEMBL | Antagonist activity against CRTh2 receptor in human whole blood assessed as eosinophil shape change | F | 6.71 | pIC50 | 195 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4794-4798 [PMID:19592244] |
ChEMBL | Antagonist activity at human CRTH2 receptor assessed as inhibition of DK-PGD2-induced eosinophil chemotaxis | F | 6.77 | pIC50 | 169 | nM | IC50 | J Med Chem (2008) 51: 2227-2243 [PMID:18318469] |
ChEMBL | Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (2011) 54: 1779-1788 [PMID:21355602] |
ChEMBL | Inhibition of PGD2-induced inositol phosphate formation at human chemoattractant receptor-homologous molecule expressed on TH2 cells | F | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Inhibition of beta-arrestin translocation at human chemoattractant receptor-homologous molecule expressed on TH2 cells in BRET assay | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Antagonist activity against CRTh2 receptor in human eosinophils assessed as cell shape change | F | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4794-4798 [PMID:19592244] |
DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - | J Biol Chem (2005) 280: 32442-32451 [PMID:16030019] |
DP2 receptor in Rat [GtoPdb: 339] [UniProtKB: Q6XKD3] | ||||||||
GtoPdb | - | - | 7.3 | pIC50 | - | - | - | J Pharmacol Exp Ther (2003) 307: 518-25 [PMID:12975488] |
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
ChEMBL | Binding affinity to prostanoid DP1 receptor | B | 4.96 | pKi | 11020 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 288-293 [PMID:21106375] |
ChEMBL | Inhibition of [3H]-PGD-2 binding to human Prostaglandin D2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Displacement of [3H]PGD2 from prostaglandin D1 receptor in human platelet membrane | B | 4.48 | pIC50 | 33400 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
ChEMBL | Inhibition of PGD2-induced inositol phosphate formation at human Prostaglandin D2 receptor | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
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 | pIC50 | >100000 | 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 | Inhibitory activity for binding of PGD-2 in hTP binding assay using HEK293 cell membranes | F | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1749-1753 [PMID:15745833] |
GtoPdb | - | - | 8 | pKi | - | - | - | Biochem Pharmacol (1992) 44: 495-503 [PMID:1387312] |
ChEMBL | Inhibition of [3H]SQ-29,548 binding to human Thromboxane A2 receptor | B | 8.35 | pKi | 4.5 | nM | Ki | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Binding affinity to thromboxane receptor | B | 9.24 | pKi | 0.58 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 288-293 [PMID:21106375] |
ChEMBL | Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4647-4651 [PMID:19608418] |
ChEMBL | Inhibition of U-46,619-induced inositol phosphate accumulation at human Thromboxane A2 receptor | F | 8.02 | pIC50 | 9.6 | nM | IC50 | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL | Inhibition of beta-arrestin translocation at human Thromboxane A2 receptor in BRET assay | F | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2005) 48: 897-900 [PMID:15715457] |
ChEMBL data shown on this page come from version 32:
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]