ramatroban [Ligand Id: 1911] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL361812 (Baynas, BAY U 3405, BAY-U-3405, EN 137774, EN-137774, Ramatroban)
  • DP2 receptor/G protein-coupled receptor 44 in Human [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
  • DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
  • DP2 receptor in Rat [GtoPdb: 339] [UniProtKB: Q6XKD3]
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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]
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 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]