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Assay Detail

CHEMBL4201008

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

Binding
Inhibition of ACK1 (unknown origin) by radiometric biochemical kinase assay
30
Total Activities
30
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

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T.
J Med Chem (2018) 61 : 8353 -8373
PubMed 30153003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.64 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4207036 1 8.22
CHEMBL4214342 1 8.10
CHEMBL4213673 1 8.05
CHEMBL4212150 1 8.00
CHEMBL4212663 1 7.96
CHEMBL4202685 1 7.89
CHEMBL4215916 1 7.82
CHEMBL459850 1 7.75
CHEMBL4209948 1 7.70
CHEMBL4212809 1 7.70
CHEMBL4217421 1 7.70
CHEMBL4209082 1 7.68
CHEMBL4213019 1 7.68
CHEMBL4215989 1 7.68
CHEMBL4203337 1 7.64
CHEMBL4207753 1 7.60
CHEMBL1214141 1 7.60
CHEMBL4216786 1 7.60
CHEMBL4218831 1 7.58
CHEMBL4207100 1 7.58
CHEMBL4211976 1 7.55
CHEMBL4214863 1 7.55
CHEMBL4210482 1 7.46
CHEMBL4213945 1 7.44
CHEMBL1214142 1 7.43
CHEMBL4206139 1 7.40
CHEMBL4205942 1 7.40
CHEMBL4211880 1 7.28
CHEMBL4211395 1 7.22
CHEMBL4210185 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4207036 IC50 = 6.0 nM 8.22
CHEMBL4214342 IC50 = 8.0 nM 8.10
CHEMBL4213673 IC50 = 9.0 nM 8.05
CHEMBL4212150 IC50 = 10.0 nM 8.00
CHEMBL4212663 IC50 = 11.0 nM 7.96
CHEMBL4202685 IC50 = 13.0 nM 7.89
CHEMBL4215916 IC50 = 15.0 nM 7.82
CHEMBL459850 IC50 = 18.0 nM 7.75
CHEMBL4209948 IC50 = 20.0 nM 7.70
CHEMBL4212809 IC50 = 20.0 nM 7.70
CHEMBL4217421 IC50 = 20.0 nM 7.70
CHEMBL4209082 IC50 = 21.0 nM 7.68
CHEMBL4213019 IC50 = 21.0 nM 7.68
CHEMBL4215989 IC50 = 21.0 nM 7.68
CHEMBL4203337 IC50 = 23.0 nM 7.64
CHEMBL4207753 IC50 = 25.0 nM 7.60
CHEMBL1214141 IC50 = 25.0 nM 7.60
CHEMBL4216786 IC50 = 25.0 nM 7.60
CHEMBL4218831 IC50 = 26.0 nM 7.58
CHEMBL4207100 IC50 = 26.0 nM 7.58
CHEMBL4211976 IC50 = 28.0 nM 7.55
CHEMBL4214863 IC50 = 28.0 nM 7.55
CHEMBL4210482 IC50 = 35.0 nM 7.46
CHEMBL4213945 IC50 = 36.0 nM 7.44
CHEMBL1214142 IC50 = 37.0 nM 7.43
CHEMBL4206139 IC50 = 40.0 nM 7.40
CHEMBL4205942 IC50 = 40.0 nM 7.40
CHEMBL4211880 IC50 = 53.0 nM 7.28
CHEMBL4211395 IC50 = 60.0 nM 7.22
CHEMBL4210185 IC50 = 94.0 nM 7.03