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Assay Detail

CHEMBL3389954

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
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
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.
Itadani S, Takahashi S, Ima M, Sekiguchi T, Fujita M, Nakayama Y, Takeuchi J.
ACS Med Chem Lett (2014) 5 : 1230 -1234
PubMed 25408836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.89 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342952 1 8.85
CHEMBL3342955 1 7.96
CHEMBL3342954 1 7.92
CHEMBL3342950 1 7.89
CHEMBL3342964 1 7.77
CHEMBL3342962 1 7.50
CHEMBL3342956 1 7.36
CHEMBL3342963 1 7.29
CHEMBL3342947 1 7.27
CHEMBL3342959 1 6.92
CHEMBL3342957 1 6.89
CHEMBL3342951 1 6.82
CHEMBL3342961 1 6.54
CHEMBL3341770 1 6.52
CHEMBL285954 1 6.36
CHEMBL3342949 1 6.08
CHEMBL3342958 1 5.89
CHEMBL3342960 1 5.52
CHEMBL3342948 1 5.34
CHEMBL3342946 1 5.01
CHEMBL3342944 1 -
CHEMBL3342945 1 -
CHEMBL3342953 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342952 IC50 = 1.4 nM 8.85
CHEMBL3342955 IC50 = 11.0 nM 7.96
CHEMBL3342954 IC50 = 12.0 nM 7.92
CHEMBL3342950 IC50 = 13.0 nM 7.89
CHEMBL3342964 IC50 = 17.0 nM 7.77
CHEMBL3342962 IC50 = 32.0 nM 7.50
CHEMBL3342956 IC50 = 44.0 nM 7.36
CHEMBL3342963 IC50 = 51.0 nM 7.29
CHEMBL3342947 IC50 = 54.0 nM 7.27
CHEMBL3342959 IC50 = 120.0 nM 6.92
CHEMBL3342957 IC50 = 130.0 nM 6.89
CHEMBL3342951 IC50 = 150.0 nM 6.82
CHEMBL3342961 IC50 = 290.0 nM 6.54
CHEMBL3341770 IC50 = 300.0 nM 6.52
CHEMBL285954 IC50 = 440.0 nM 6.36
CHEMBL3342949 IC50 = 840.0 nM 6.08
CHEMBL3342958 IC50 = 1300.0 nM 5.89
CHEMBL3342960 IC50 = 3000.0 nM 5.52
CHEMBL3342948 IC50 = 4600.0 nM 5.34
CHEMBL3342946 IC50 = 9700.0 nM 5.01
CHEMBL3342944 IC50 > 10000.0 nM -
CHEMBL3342945 IC50 > 2500.0 nM -
CHEMBL3342953 IC50 < 1.0 nM -