[3H]ramatroban [Ligand Id: 1910] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL361812 (EN 137774, EN-137774, BAY U 3405, BAY-U-3405, Ramatroban)
  • DP2 receptor/G protein-coupled receptor 44 in Human [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
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  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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  • TP receptor/Thromboxane A2 receptor in Human [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
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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]
GtoPdb - - 8.1 pKd - - - Eur J Pharmacol (2005) 524: 30-7 [PMID:16256979]
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]
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]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]