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Assay Detail

CHEMBL903616

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Binding
Inhibition of Ack1
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Activated CDC42 kinase 1 (CHEMBL4599)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.
Martin MW, Newcomb J, Nunes JJ, Bemis JE, McGowan DC, White RD, Buchanan JL, DiMauro EF, Boucher C, Faust T, Hsieh F, Huang X, Lee JH, Schneider S, Turci SM, Zhu X.
Bioorg Med Chem Lett (2007) 17 : 2299 -2304
PubMed 17276681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.82 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437754 1 7.70
CHEMBL240432 1 7.08
CHEMBL240429 1 6.96
CHEMBL393596 1 6.92
CHEMBL240430 1 6.82
CHEMBL240431 1 6.77
CHEMBL427687 1 6.75
CHEMBL239590 1 6.75
CHEMBL392990 1 6.38
CHEMBL239591 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437754 IC50 = 20.0 nM 7.70
CHEMBL240432 IC50 = 84.0 nM 7.08
CHEMBL240429 IC50 = 110.0 nM 6.96
CHEMBL393596 IC50 = 120.0 nM 6.92
CHEMBL240430 IC50 = 150.0 nM 6.82
CHEMBL240431 IC50 = 170.0 nM 6.77
CHEMBL427687 IC50 = 180.0 nM 6.75
CHEMBL239590 IC50 = 180.0 nM 6.75
CHEMBL392990 IC50 = 420.0 nM 6.38
CHEMBL239591 IC50 = 930.0 nM 6.03