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Assay Detail

CHEMBL1909164

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Binding
DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 6.02 8.76
Ki 871 6.32 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603 ZAFIRLUKAST 4.0 2 9.06
CHEMBL787 MONTELUKAST 4.0 2 8.94
CHEMBL434063 2 5.26
CHEMBL411 DIETHYLSTILBESTROL 4.0 2 5.05
CHEMBL18797 SULINDAC SULFIDE -1.0 2 4.83
CHEMBL104 CLOTRIMAZOLE 4.0 2 4.78
CHEMBL894 BUPROPION 4.0 2 -
CHEMBL49 BUSPIRONE 4.0 2 -
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 2 -
CHEMBL277474 ANTIPYRINE 3.0 2 -
CHEMBL24 ATENOLOL 4.0 2 -
CHEMBL1598608 AZASETRON 2.0 2 -
CHEMBL1201346 BALSALAZIDE 4.0 2 -
CHEMBL31184 BENZO[DEF]CHRYSENE 0.5 2 -
CHEMBL415690 BETADEX 3.0 2 -
CHEMBL264374 BEZAFIBRATE 3.0 2 -
CHEMBL108 CARBAMAZEPINE 4.0 2 -
CHEMBL253376 BROMHEXINE 3.0 2 -
CHEMBL1077 BROMFENAC 4.0 2 -
CHEMBL1231530 BETAMIPRON 2.0 2 -
CHEMBL12089 BERBERINE CHLORIDE 1.0 2 -
CHEMBL221753 BENZETHONIUM CHLORIDE 2.0 2 -
CHEMBL701 BACLOFEN 4.0 2 -
CHEMBL1095699 AZASERINE 2.0 2 -
CHEMBL3084803 ASTROMICIN 2.0 2 -
CHEMBL211501 ANTIMYCIN A 2 -
CHEMBL14 CARBACHOL 4.0 2 -
CHEMBL1458880 CADMIUM DICHLORIDE 2 -
CHEMBL1200396 BUPIVACAINE HYDROCHLORIDE 4.0 2 -
CHEMBL844 BRIMONIDINE 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603 ZAFIRLUKAST Ki = 0.865 nM 9.06
CHEMBL787 MONTELUKAST Ki = 1.143 nM 8.94
CHEMBL603 ZAFIRLUKAST IC50 = 1.731 nM 8.76
CHEMBL787 MONTELUKAST IC50 = 2.287 nM 8.64
CHEMBL434063 Ki = 5455.0 nM 5.26
CHEMBL411 DIETHYLSTILBESTROL Ki = 8872.0 nM 5.05
CHEMBL434063 IC50 = 10910.0 nM 4.96
CHEMBL18797 SULINDAC SULFIDE Ki = 14684.0 nM 4.83
CHEMBL104 CLOTRIMAZOLE Ki = 16586.0 nM 4.78
CHEMBL411 DIETHYLSTILBESTROL IC50 = 17745.0 nM 4.75
CHEMBL18797 SULINDAC SULFIDE IC50 = 29368.0 nM 4.53
CHEMBL104 CLOTRIMAZOLE IC50 = 33172.0 nM 4.48
CHEMBL2106399 KITASAMYCIN Ki - -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 Ki - -
CHEMBL741 LAMOTRIGINE IC50 - -
CHEMBL741 LAMOTRIGINE Ki - -
CHEMBL1373 MODAFINIL Ki - -
CHEMBL1513 IRBESARTAN Ki - -
CHEMBL1513 IRBESARTAN IC50 - -
CHEMBL80 NALOXONE Ki - -
CHEMBL80 NALOXONE IC50 - -
CHEMBL91 MICONAZOLE Ki - -
CHEMBL91 MICONAZOLE IC50 - -
CHEMBL878 METOLAZONE Ki - -
CHEMBL878 METOLAZONE IC50 - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER Ki - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER IC50 - -
CHEMBL164290 N-NITROSODIETHYLAMINE Ki - -
CHEMBL164290 N-NITROSODIETHYLAMINE IC50 - -
CHEMBL503 LOVASTATIN Ki - -
CHEMBL503 LOVASTATIN IC50 - -
CHEMBL86 METOCLOPRAMIDE Ki - -
CHEMBL86304 MOCLOBEMIDE Ki - -
CHEMBL975 MESNA IC50 - -
CHEMBL1630579 MYRTECAINE IC50 - -
CHEMBL1630579 MYRTECAINE Ki - -
CHEMBL19019 NALTREXONE IC50 - -
CHEMBL19019 NALTREXONE Ki - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki - -
CHEMBL86 METOCLOPRAMIDE IC50 - -
CHEMBL2106399 KITASAMYCIN IC50 - -
CHEMBL6437 MIANSERIN IC50 - -
CHEMBL6437 MIANSERIN Ki - -
CHEMBL1618305 NALOXONAZINE IC50 - -
CHEMBL1618305 NALOXONAZINE Ki - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL92401 IPRONIAZID Ki - -
CHEMBL64391 ITRACONAZOLE IC50 - -
CHEMBL64391 ITRACONAZOLE Ki - -