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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] | ||||||||
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 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]