Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2090703

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

Binding
Inhibition of N-terminal His6-tagged ACK1 expressed in baculovirus infected Hi5 cells assessed as inhibition of autophosphorylation after 2 hrs by ELISA
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type BTI-TN-5B1-4
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.
Jiao X, Kopecky DJ, Liu J, Liu J, Jaen JC, Cardozo MG, Sharma R, Walker N, Wesche H, Li S, Farrelly E, Xiao SH, Wang Z, Kayser F.
Bioorg Med Chem Lett (2012) 22 : 6212 -6217
PubMed 22929232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 7.98 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2087874 1 9.70
CHEMBL2087875 1 9.52
CHEMBL2087873 1 9.52
CHEMBL2087652 1 8.70
CHEMBL2087654 1 8.70
CHEMBL2087662 1 8.70
CHEMBL2087664 1 8.52
CHEMBL2087879 1 8.40
CHEMBL2087659 1 8.40
CHEMBL2087660 1 8.40
CHEMBL2087656 1 8.40
CHEMBL2087653 1 8.40
CHEMBL2087872 1 8.40
CHEMBL2087648 1 8.30
CHEMBL247479 1 8.30
CHEMBL2087658 1 8.22
CHEMBL2087647 1 8.22
CHEMBL2087649 1 8.22
CHEMBL2087666 1 8.22
CHEMBL2087665 1 8.22
CHEMBL2087655 1 8.22
CHEMBL2087657 1 8.22
CHEMBL2087651 1 8.15
CHEMBL2087876 1 8.10
CHEMBL2087650 1 8.10
CHEMBL2087661 1 8.00
CHEMBL2087671 1 8.00
CHEMBL2087667 1 8.00
CHEMBL2087877 1 7.89
CHEMBL2087663 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2087874 Ki = 0.2 nM 9.70
CHEMBL2087875 Ki = 0.3 nM 9.52
CHEMBL2087873 Ki = 0.3 nM 9.52
CHEMBL2087652 Ki = 2.0 nM 8.70
CHEMBL2087654 Ki = 2.0 nM 8.70
CHEMBL2087662 Ki = 2.0 nM 8.70
CHEMBL2087664 Ki = 3.0 nM 8.52
CHEMBL2087659 Ki = 4.0 nM 8.40
CHEMBL2087660 Ki = 4.0 nM 8.40
CHEMBL2087656 Ki = 4.0 nM 8.40
CHEMBL2087879 Ki = 4.0 nM 8.40
CHEMBL2087653 Ki = 4.0 nM 8.40
CHEMBL2087872 Ki = 4.0 nM 8.40
CHEMBL2087648 Ki = 5.0 nM 8.30
CHEMBL247479 Ki = 5.0 nM 8.30
CHEMBL2087658 Ki = 6.0 nM 8.22
CHEMBL2087657 Ki = 6.0 nM 8.22
CHEMBL2087655 Ki = 6.0 nM 8.22
CHEMBL2087665 Ki = 6.0 nM 8.22
CHEMBL2087666 Ki = 6.0 nM 8.22
CHEMBL2087649 Ki = 6.0 nM 8.22
CHEMBL2087647 Ki = 6.0 nM 8.22
CHEMBL2087651 Ki = 7.0 nM 8.15
CHEMBL2087650 Ki = 8.0 nM 8.10
CHEMBL2087876 Ki = 8.0 nM 8.10
CHEMBL2087661 Ki = 10.0 nM 8.00
CHEMBL2087671 Ki = 10.0 nM 8.00
CHEMBL2087667 Ki = 10.0 nM 8.00
CHEMBL2087877 Ki = 13.0 nM 7.89
CHEMBL2087663 Ki = 13.0 nM 7.89
CHEMBL2087881 Ki = 20.0 nM 7.70
CHEMBL2087668 Ki = 20.0 nM 7.70
CHEMBL2087871 Ki = 20.0 nM 7.70
CHEMBL2087880 Ki = 30.0 nM 7.52
CHEMBL2087670 Ki = 40.0 nM 7.40
CHEMBL2087882 Ki = 40.0 nM 7.40
CHEMBL2087883 Ki = 50.0 nM 7.30
CHEMBL2087884 Ki = 50.0 nM 7.30
CHEMBL2087878 Ki = 69.0 nM 7.16
CHEMBL240429 Ki = 70.0 nM 7.16
CHEMBL2087887 Ki = 1800.0 nM 5.75
CHEMBL2087669 Ki = 1980.0 nM 5.70
CHEMBL2087886 Ki = 7300.0 nM 5.14
CHEMBL2087885 Ki > 10000.0 nM -