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Assay Detail

CHEMBL1909206

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

Binding
DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Insect cells
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Lck (CHEMBL258)
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 5.31 7.10
Ki 871 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506247 TANNIC ACID 4.0 2 7.10
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 2 6.53
CHEMBL1476898 CADMIUM ACETATE 2 6.08
CHEMBL1201469 GRAMICIDIN 4.0 2 5.96
CHEMBL12131 CLOSANTEL 2.0 2 5.90
CHEMBL1200558 BACITRACIN 4.0 2 5.72
CHEMBL290106 BITHIONOL 4.0 2 5.65
CHEMBL496 HEXACHLOROPHENE 4.0 2 5.61
CHEMBL86754 IODOQUINOL 2.0 2 5.61
CHEMBL1386 TRANSPLATIN 3.0 2 5.57
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 2 5.54
CHEMBL334255 CETYLPYRIDINIUM BROMIDE 2 5.50
CHEMBL1009 LEVODOPA 4.0 2 5.43
CHEMBL24944 TRIBROMSALAN 4.0 2 5.30
CHEMBL926 DOBUTAMINE 4.0 2 5.26
CHEMBL442 ERGOTAMINE 4.0 2 5.19
CHEMBL1200748 CARBIDOPA 4.0 2 5.17
CHEMBL83 TAMOXIFEN 4.0 2 5.09
CHEMBL1630578 TIRILAZAD 3.0 2 4.80
CHEMBL141343 2 4.77
CHEMBL1201631 INSULIN HUMAN 4.0 2 4.74
CHEMBL296419 ASTEMIZOLE 4.0 2 4.70
CHEMBL195437 4-OCTYLPHENOL 2 4.66
CHEMBL11359 CISPLATIN 4.0 2 4.64
CHEMBL53463 DOXORUBICIN 4.0 2 4.50
CHEMBL40583 3-METHYLCHOLANTHRENE 2 4.26
CHEMBL584 NELFINAVIR 4.0 2 4.10
CHEMBL515914 AZARIBINE 4.0 2 -
CHEMBL388590 BENZBROMARONE 4.0 2 -
CHEMBL720 BENZYL ALCOHOL 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506247 TANNIC ACID IC50 = 79.0 nM 7.10
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 IC50 = 293.8 nM 6.53
CHEMBL1476898 CADMIUM ACETATE IC50 = 824.0 nM 6.08
CHEMBL1201469 GRAMICIDIN IC50 = 1094.0 nM 5.96
CHEMBL12131 CLOSANTEL IC50 = 1249.0 nM 5.90
CHEMBL1200558 BACITRACIN IC50 = 1923.0 nM 5.72
CHEMBL290106 BITHIONOL IC50 = 2255.0 nM 5.65
CHEMBL86754 IODOQUINOL IC50 = 2461.0 nM 5.61
CHEMBL496 HEXACHLOROPHENE IC50 = 2432.5 nM 5.61
CHEMBL1386 TRANSPLATIN IC50 = 2721.0 nM 5.57
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER IC50 = 2887.0 nM 5.54
CHEMBL334255 CETYLPYRIDINIUM BROMIDE IC50 = 3182.0 nM 5.50
CHEMBL1009 LEVODOPA IC50 = 3729.0 nM 5.43
CHEMBL24944 TRIBROMSALAN IC50 = 5015.0 nM 5.30
CHEMBL926 DOBUTAMINE IC50 = 5519.0 nM 5.26
CHEMBL442 ERGOTAMINE IC50 = 6499.0 nM 5.19
CHEMBL1200748 CARBIDOPA IC50 = 6795.0 nM 5.17
CHEMBL83 TAMOXIFEN IC50 = 8033.0 nM 5.09
CHEMBL1630578 TIRILAZAD IC50 = 15786.0 nM 4.80
CHEMBL141343 IC50 = 17137.0 nM 4.77
CHEMBL1201631 INSULIN HUMAN IC50 = 18107.0 nM 4.74
CHEMBL296419 ASTEMIZOLE IC50 = 19920.0 nM 4.70
CHEMBL195437 4-OCTYLPHENOL IC50 = 22054.0 nM 4.66
CHEMBL11359 CISPLATIN IC50 = 22949.0 nM 4.64
CHEMBL53463 DOXORUBICIN IC50 = 31913.0 nM 4.50
CHEMBL40583 3-METHYLCHOLANTHRENE IC50 = 55452.0 nM 4.26
CHEMBL584 NELFINAVIR IC50 = 79166.0 nM 4.10
CHEMBL21731 MAPROTILINE IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL1618305 NALOXONAZINE Ki - -
CHEMBL558 MEXILETINE IC50 - -
CHEMBL741 LAMOTRIGINE Ki - -
CHEMBL741 LAMOTRIGINE IC50 - -
CHEMBL2106399 KITASAMYCIN Ki - -
CHEMBL1630579 MYRTECAINE Ki - -
CHEMBL1630579 MYRTECAINE IC50 - -
CHEMBL86304 MOCLOBEMIDE Ki - -
CHEMBL86304 MOCLOBEMIDE IC50 - -
CHEMBL21731 MAPROTILINE Ki - -
CHEMBL503 LOVASTATIN IC50 - -
CHEMBL191 LOSARTAN Ki - -
CHEMBL503 LOVASTATIN Ki - -
CHEMBL1909067 IC50 - -
CHEMBL191 LOSARTAN IC50 - -
CHEMBL1909067 Ki - -
CHEMBL534 KETOTIFEN Ki - -
CHEMBL91 MICONAZOLE IC50 - -
CHEMBL91 MICONAZOLE Ki - -
CHEMBL534 KETOTIFEN IC50 - -
CHEMBL1201237 LEVOBUNOLOL IC50 - -