BAYu9773 [Ligand Id: 3381] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL285954 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271] | ||||||||
| GtoPdb | - | - | 5.3 | pIC50 | 5000 | nM | IC50 | Br J Pharmacol (2010) 160: 399-409 [PMID:20423349] |
| ChEMBL | Antagonist activity at human CysLT1 receptor expressed in CHO cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay | F | 6.36 | pIC50 | 440 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1230-1234 [PMID:25408836] |
| GtoPdb | - | - | 6.36 | pIC50 | 440 | nM | IC50 | Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801] |
| Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity on guinea-pig ileum | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1517-1522 |
| CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75] | ||||||||
| GtoPdb | - | - | 5.34 | pIC50 | 4600 | nM | IC50 | J Pharmacol Exp Ther (2011) 339: 768-78 [PMID:21903747] |
| GtoPdb | - | - | 6.4 | pIC50 | 400 | nM | IC50 |
J Biol Chem (2000) 275: 30531-6 [PMID:10851239]; Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]; Br J Pharmacol (2010) 160: 399-409 [PMID:20423349] |
| GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801] |
| ChEMBL | Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay | F | 6.52 | pIC50 | 300 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1230-1234 [PMID:25408836] |
| GtoPdb | - | - | 7.74 | pIC50 | 18 | nM | IC50 | Br J Pharmacol (2010) 160: 399-409 [PMID:20423349] |
| GtoPdb | - | - | 7.04 | pEC50 | 92 | nM | EC50 | Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801] |
| GtoPdb | - | - | 7.16 | pEC50 | 69 | nM | EC50 | Br J Pharmacol (2010) 160: 399-409 [PMID:20423349] |
| CysLT2 receptor in Rat [GtoPdb: 270] [UniProtKB: Q924T9] | ||||||||
| GtoPdb | against LTC4 and LTD4 induced contraction in smooth muscle preparation | - | 7.7 | pA2 | - | - | - | Eur J Pharmacol (1994) 264: 317-323 [PMID:7698171] |
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]
