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Assay Detail

CHEMBL1017265

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

Binding
Inhibition of histidine-tagged ACK1 (amino acids 117 to 489) expressed in SF9 cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
Kopecky DJ, Hao X, Chen Y, Fu J, Jiao X, Jaen JC, Cardozo MG, Liu J, Wang Z, Walker NP, Wesche H, Li S, Farrelly E, Xiao SH, Kayser F.
Bioorg Med Chem Lett (2008) 18 : 6352 -6356
PubMed 18993068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.85 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487897 1 8.70
CHEMBL504331 1 8.70
CHEMBL472392 1 8.70
CHEMBL487242 1 8.52
CHEMBL458333 1 8.52
CHEMBL502156 1 8.52
CHEMBL450918 1 8.52
CHEMBL487054 1 8.30
CHEMBL487241 1 8.30
CHEMBL487243 1 8.15
CHEMBL461159 1 8.00
CHEMBL488061 1 8.00
CHEMBL462189 1 8.00
CHEMBL459220 1 7.92
CHEMBL487896 1 7.92
CHEMBL514919 1 7.75
CHEMBL459044 1 7.70
CHEMBL521379 1 7.58
CHEMBL461337 1 7.52
CHEMBL520403 1 7.52
CHEMBL488062 1 7.52
CHEMBL521381 1 7.52
CHEMBL487055 1 7.40
CHEMBL462364 1 7.30
CHEMBL518822 1 7.30
CHEMBL519916 1 7.16
CHEMBL462365 1 7.10
CHEMBL461158 1 7.00
CHEMBL516660 1 6.40
CHEMBL487048 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487897 Ki = 2.0 nM 8.70
CHEMBL504331 Ki = 2.0 nM 8.70
CHEMBL472392 Ki = 2.0 nM 8.70
CHEMBL487242 Ki = 3.0 nM 8.52
CHEMBL458333 Ki = 3.0 nM 8.52
CHEMBL502156 Ki = 3.0 nM 8.52
CHEMBL450918 Ki = 3.0 nM 8.52
CHEMBL487054 Ki = 5.0 nM 8.30
CHEMBL487241 Ki = 5.0 nM 8.30
CHEMBL487243 Ki = 7.0 nM 8.15
CHEMBL461159 Ki = 10.0 nM 8.00
CHEMBL488061 Ki = 10.0 nM 8.00
CHEMBL462189 Ki = 10.0 nM 8.00
CHEMBL459220 Ki = 12.0 nM 7.92
CHEMBL487896 Ki = 12.0 nM 7.92
CHEMBL514919 Ki = 18.0 nM 7.75
CHEMBL459044 Ki = 20.0 nM 7.70
CHEMBL521379 Ki = 26.0 nM 7.58
CHEMBL461337 Ki = 30.0 nM 7.52
CHEMBL520403 Ki = 30.0 nM 7.52
CHEMBL488062 Ki = 30.0 nM 7.52
CHEMBL521381 Ki = 30.0 nM 7.52
CHEMBL487055 Ki = 40.0 nM 7.40
CHEMBL462364 Ki = 50.0 nM 7.30
CHEMBL518822 Ki = 50.0 nM 7.30
CHEMBL519916 Ki = 70.0 nM 7.16
CHEMBL462365 Ki = 80.0 nM 7.10
CHEMBL461158 Ki = 100.0 nM 7.00
CHEMBL516660 Ki = 400.0 nM 6.40
CHEMBL487048 Ki > 2500.0 nM -
CHEMBL472393 Ki > 4000.0 nM -