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 33:
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]
