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Assay Detail

CHEMBL5265489

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

Binding
Inhibition of ACK1 (unknown origin)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Small Molecules Targeting Activated Cdc42-Associated Kinase 1 (ACK1/TNK2) for the Treatment of Cancers.
Wang A, Pei J, Shuai W, Lin C, Feng L, Wang Y, Lin F, Ouyang L, Wang G.
J Med Chem (2021) 64 : 16328 -16348
PubMed 34735773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.39 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 9.00
CHEMBL288441 BOSUTINIB 4.0 1 8.57
CHEMBL1229517 VEMURAFENIB 4.0 1 7.72
CHEMBL2403108 CERITINIB 4.0 1 7.47
CHEMBL3353410 OSIMERTINIB 4.0 1 7.15
CHEMBL53753 1 6.70
CHEMBL535 SUNITINIB 4.0 1 5.11
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL428690 ALVOCIDIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 1.0 nM 9.00
CHEMBL288441 BOSUTINIB IC50 = 2.7 nM 8.57
CHEMBL1229517 VEMURAFENIB IC50 = 19.0 nM 7.72
CHEMBL2403108 CERITINIB IC50 = 33.6 nM 7.47
CHEMBL3353410 OSIMERTINIB IC50 = 71.0 nM 7.15
CHEMBL53753 IC50 = 200.0 nM 6.70
CHEMBL535 SUNITINIB IC50 = 7830.0 nM 5.11
CHEMBL939 GEFITINIB IC50 < 20000.0 nM -
CHEMBL428690 ALVOCIDIB IC50 < 20000.0 nM -