Assay Detail

CHEMBL3599869

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Binding

Antagonist activity at human CysLT1

ChEMBL ↗

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Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798) ↗

Open DB target context

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Cysteinyl leukotriene receptor 1 (CHEMBL1798) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cysteinyl leukotriene receptor 1

CHEMBL1798

Anchored from Assay target.

Protein identity Cysteinyl leukotriene receptor 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.

Itadani S, Yashiro K, Aratani Y, Sekiguchi T, Kinoshita A, Moriguchi H, Ohta N, Takahashi S, Ishida A, Tajima Y, Hisaichi K, Ima M, Ueda J, Egashira H, Sekioka T, Kadode M, Yonetomi Y, Nakao T, Inoue A, Nomura H, Kitamine T, Fujita M, Nabe T, Yamaura Y, Matsumura N, Imagawa A, Nakayama Y, Takeuchi J, Ohmoto K.
J Med Chem (2015) 58 : 6093 -6113
PubMed 26200813 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	8.58	8.72

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL603	ZAFIRLUKAST	4.0	1	8.72
CHEMBL787	MONTELUKAST	4.0	1	8.64
CHEMBL21333	PRANLUKAST	4.0	1	8.37

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL603	ZAFIRLUKAST	IC50	=	1.9	nM	8.72
CHEMBL787	MONTELUKAST	IC50	=	2.3	nM	8.64
CHEMBL21333	PRANLUKAST	IC50	=	4.3	nM	8.37