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Assay Detail

CHEMBL1909215

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

Binding
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
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

Adenosine receptor A3 (CHEMBL256)
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 5.46 7.02
Ki 871 5.71 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12131 CLOSANTEL 2.0 2 7.27
CHEMBL1289 HALOPROGIN 4.0 2 6.90
CHEMBL508112 BENZOTHIAZYL DISULFIDE 2 6.71
CHEMBL964 DISULFIRAM 4.0 2 6.70
CHEMBL787 MONTELUKAST 4.0 2 6.61
CHEMBL6067487 IVERMECTIN 4.0 2 6.54
CHEMBL1262 OXICONAZOLE 4.0 2 6.45
CHEMBL496 HEXACHLOROPHENE 4.0 2 6.44
CHEMBL290106 BITHIONOL 4.0 2 6.33
CHEMBL3215298 ABAMECTIN 3.0 2 6.31
CHEMBL86754 IODOQUINOL 2.0 2 6.28
CHEMBL1386 TRANSPLATIN 3.0 2 6.25
CHEMBL1480 FELODIPINE 4.0 2 6.22
CHEMBL1016 CANDESARTAN 3.0 2 6.16
CHEMBL603 ZAFIRLUKAST 4.0 2 6.11
CHEMBL306043 GOLD SODIUM THIOMALATE 2.0 2 6.07
CHEMBL1366 AURANOFIN 4.0 2 6.02
CHEMBL153062 4-NONYLPHENOL 2 5.97
CHEMBL411 DIETHYLSTILBESTROL 4.0 2 5.90
CHEMBL1221 SULCONAZOLE 4.0 2 5.83
CHEMBL91 MICONAZOLE 4.0 2 5.80
CHEMBL7002 CIGLITAZONE 2.0 2 5.76
CHEMBL305660 EBASTINE 4.0 2 5.74
CHEMBL808 ECONAZOLE 4.0 2 5.74
CHEMBL1219 RABEPRAZOLE 4.0 2 5.74
CHEMBL508338 THIMEROSAL 3.0 2 5.72
CHEMBL83 TAMOXIFEN 4.0 2 5.68
CHEMBL404849 SULOCTIDIL 4.0 2 5.68
CHEMBL460291 LACIDIPINE 3.0 2 5.64
CHEMBL64894 GENTIAN VIOLET 4.0 2 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12131 CLOSANTEL Ki = 54.0 nM 7.27
CHEMBL12131 CLOSANTEL IC50 = 96.0 nM 7.02
CHEMBL1289 HALOPROGIN Ki = 126.0 nM 6.90
CHEMBL508112 BENZOTHIAZYL DISULFIDE Ki = 196.0 nM 6.71
CHEMBL964 DISULFIRAM Ki = 201.0 nM 6.70
CHEMBL1289 HALOPROGIN IC50 = 223.0 nM 6.65
CHEMBL787 MONTELUKAST Ki = 245.0 nM 6.61
CHEMBL6067487 IVERMECTIN Ki = 289.4 nM 6.54
CHEMBL508112 BENZOTHIAZYL DISULFIDE IC50 = 347.0 nM 6.46
CHEMBL1262 OXICONAZOLE Ki = 358.6 nM 6.45
CHEMBL964 DISULFIRAM IC50 = 356.0 nM 6.45
CHEMBL496 HEXACHLOROPHENE Ki = 361.1 nM 6.44
CHEMBL787 MONTELUKAST IC50 = 434.0 nM 6.36
CHEMBL290106 BITHIONOL Ki = 468.0 nM 6.33
CHEMBL3215298 ABAMECTIN Ki = 492.0 nM 6.31
CHEMBL6067487 IVERMECTIN IC50 = 512.1 nM 6.29
CHEMBL86754 IODOQUINOL Ki = 527.0 nM 6.28
CHEMBL1386 TRANSPLATIN Ki = 559.0 nM 6.25
CHEMBL1480 FELODIPINE Ki = 597.0 nM 6.22
CHEMBL1262 OXICONAZOLE IC50 = 634.5 nM 6.20
CHEMBL496 HEXACHLOROPHENE IC50 = 638.9 nM 6.20
CHEMBL1016 CANDESARTAN Ki = 689.5 nM 6.16
CHEMBL603 ZAFIRLUKAST Ki = 770.0 nM 6.11
CHEMBL290106 BITHIONOL IC50 = 829.0 nM 6.08
CHEMBL306043 GOLD SODIUM THIOMALATE Ki = 843.0 nM 6.07
CHEMBL3215298 ABAMECTIN IC50 = 870.0 nM 6.06
CHEMBL86754 IODOQUINOL IC50 = 933.0 nM 6.03
CHEMBL1366 AURANOFIN Ki = 954.0 nM 6.02
CHEMBL1386 TRANSPLATIN IC50 = 989.1 nM 6.00
CHEMBL1480 FELODIPINE IC50 = 1057.0 nM 5.98
CHEMBL153062 4-NONYLPHENOL Ki = 1082.0 nM 5.97
CHEMBL1016 CANDESARTAN IC50 = 1219.9 nM 5.91
CHEMBL411 DIETHYLSTILBESTROL Ki = 1248.0 nM 5.90
CHEMBL603 ZAFIRLUKAST IC50 = 1363.0 nM 5.87
CHEMBL1221 SULCONAZOLE Ki = 1485.0 nM 5.83
CHEMBL306043 GOLD SODIUM THIOMALATE IC50 = 1492.0 nM 5.83
CHEMBL91 MICONAZOLE Ki = 1589.0 nM 5.80
CHEMBL1366 AURANOFIN IC50 = 1688.0 nM 5.77
CHEMBL7002 CIGLITAZONE Ki = 1722.0 nM 5.76
CHEMBL1219 RABEPRAZOLE Ki = 1820.0 nM 5.74
CHEMBL808 ECONAZOLE Ki = 1836.0 nM 5.74
CHEMBL305660 EBASTINE Ki = 1806.1 nM 5.74
CHEMBL508338 THIMEROSAL Ki = 1914.0 nM 5.72
CHEMBL153062 4-NONYLPHENOL IC50 = 1915.0 nM 5.72
CHEMBL83 TAMOXIFEN Ki = 2092.0 nM 5.68
CHEMBL404849 SULOCTIDIL Ki = 2094.6 nM 5.68
CHEMBL411 DIETHYLSTILBESTROL IC50 = 2208.0 nM 5.66
CHEMBL460291 LACIDIPINE Ki = 2281.0 nM 5.64
CHEMBL64894 GENTIAN VIOLET Ki = 2355.0 nM 5.63
CHEMBL547 ISOTRETINOIN Ki = 2357.0 nM 5.63