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Assay Detail

CHEMBL687342

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Functional
Inhibition of LTC4 induced smooth muscle contraction of guinea pig ileum
ChEMBL ↗
83
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cysteinyl leukotriene receptor (CHEMBL2094254) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
Nakai H, Konno M, Kosuge S, Sakuyama S, Toda M, Arai Y, Obata T, Katsube N, Miyamoto T, Okegawa T.
J Med Chem (1988) 31 : 84 -91
PubMed 3336036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 83 7.27 10.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354129 — — 1 10.51
CHEMBL21333 PRANLUKAST 4.0 1 10.36
CHEMBL171021 — — 1 10.22
CHEMBL169790 — — 1 9.96
CHEMBL354530 — — 1 9.85
CHEMBL170191 — — 1 9.80
CHEMBL172889 — — 1 9.43
CHEMBL170100 — — 1 9.33
CHEMBL83797 — — 1 9.30
CHEMBL170017 — — 1 9.17
CHEMBL312105 — — 1 9.07
CHEMBL171689 — — 1 9.02
CHEMBL171022 — — 1 8.96
CHEMBL170959 — — 1 8.89
CHEMBL422917 — — 1 8.82
CHEMBL170393 — — 1 8.70
CHEMBL81565 — — 1 8.38
CHEMBL353429 — — 1 8.37
CHEMBL172766 — — 1 8.30
CHEMBL170506 — — 1 8.28
CHEMBL311891 — — 1 8.26
CHEMBL83447 — — 1 8.26
CHEMBL312051 — — 1 8.15
CHEMBL312090 — — 1 8.13
CHEMBL80993 — — 1 8.05
CHEMBL174377 — — 1 7.96
CHEMBL82033 — — 1 7.89
CHEMBL311759 — — 1 7.85
CHEMBL78974 — — 1 7.82
CHEMBL171746 — — 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354129 — IC50 = 0.031 nM 10.51
CHEMBL21333 PRANLUKAST IC50 = 0.044 nM 10.36
CHEMBL171021 — IC50 = 0.06 nM 10.22
CHEMBL169790 — IC50 = 0.11 nM 9.96
CHEMBL354530 — IC50 = 0.14 nM 9.85
CHEMBL170191 — IC50 = 0.16 nM 9.80
CHEMBL172889 — IC50 = 0.37 nM 9.43
CHEMBL170100 — IC50 = 0.47 nM 9.33
CHEMBL83797 — IC50 = 0.5 nM 9.30
CHEMBL170017 — IC50 = 0.67 nM 9.17
CHEMBL312105 — IC50 = 0.86 nM 9.07
CHEMBL171689 — IC50 = 0.96 nM 9.02
CHEMBL171022 — IC50 = 1.1 nM 8.96
CHEMBL170959 — IC50 = 1.3 nM 8.89
CHEMBL422917 — IC50 = 1.5 nM 8.82
CHEMBL170393 — IC50 = 2.0 nM 8.70
CHEMBL81565 — IC50 = 4.2 nM 8.38
CHEMBL353429 — IC50 = 4.3 nM 8.37
CHEMBL172766 — IC50 = 5.0 nM 8.30
CHEMBL170506 — IC50 = 5.2 nM 8.28
CHEMBL311891 — IC50 = 5.5 nM 8.26
CHEMBL83447 — IC50 = 5.5 nM 8.26
CHEMBL312051 — IC50 = 7.0 nM 8.15
CHEMBL312090 — IC50 = 7.4 nM 8.13
CHEMBL80993 — IC50 = 9.0 nM 8.05
CHEMBL174377 — IC50 = 11.0 nM 7.96
CHEMBL82033 — IC50 = 13.0 nM 7.89
CHEMBL311759 — IC50 = 14.0 nM 7.85
CHEMBL78974 — IC50 = 15.0 nM 7.82
CHEMBL171746 — IC50 = 18.0 nM 7.75
CHEMBL173750 — IC50 = 20.0 nM 7.70
CHEMBL81585 — IC50 = 20.0 nM 7.70
CHEMBL354606 — IC50 = 21.0 nM 7.68
CHEMBL172404 — IC50 = 30.0 nM 7.52
CHEMBL169151 — IC50 = 32.0 nM 7.50
CHEMBL173692 — IC50 = 34.0 nM 7.47
CHEMBL171500 — IC50 = 53.0 nM 7.28
CHEMBL170521 — IC50 = 62.0 nM 7.21
CHEMBL81988 — IC50 = 70.0 nM 7.16
CHEMBL170035 — IC50 = 88.0 nM 7.06
CHEMBL169848 — IC50 = 100.0 nM 7.00
CHEMBL267976 FPL-55712 SODIUM SALT IC50 = 100.0 nM 7.00
CHEMBL81487 — IC50 = 100.0 nM 7.00
CHEMBL311277 — IC50 = 100.0 nM 7.00
CHEMBL354274 — IC50 = 120.0 nM 6.92
CHEMBL173495 — IC50 = 120.0 nM 6.92
CHEMBL170212 — IC50 = 140.0 nM 6.85
CHEMBL173279 — IC50 = 140.0 nM 6.85
CHEMBL170899 — IC50 = 150.0 nM 6.82
CHEMBL353716 — IC50 = 150.0 nM 6.82