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Assay Detail

CHEMBL4345183

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

Binding
Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged AAK1 kinase domain (31 to 396 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay
18
Total Activities
18
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

AP2-associated protein kinase 1 (CHEMBL3830)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD.
ACS Med Chem Lett (2020) 11 : 340 -345
PubMed 32184967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.76 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4571548 1 8.21
CHEMBL4534959 1 8.20
CHEMBL4531680 1 8.09
CHEMBL4516665 1 8.08
CHEMBL4535040 1 8.07
CHEMBL4452939 1 8.04
CHEMBL4452360 1 8.00
CHEMBL4552310 1 7.92
CHEMBL4470026 1 7.70
CHEMBL4473140 1 7.66
CHEMBL4542463 1 7.66
CHEMBL4593649 1 7.62
CHEMBL4522276 1 7.52
CHEMBL4447403 1 7.50
CHEMBL4472438 1 7.48
CHEMBL4582326 1 7.41
CHEMBL4561238 1 7.36
CHEMBL4534571 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4571548 Ki = 6.2 nM 8.21
CHEMBL4534959 Ki = 6.3 nM 8.20
CHEMBL4531680 Ki = 8.2 nM 8.09
CHEMBL4516665 Ki = 8.3 nM 8.08
CHEMBL4535040 Ki = 8.5 nM 8.07
CHEMBL4452939 Ki = 9.1 nM 8.04
CHEMBL4452360 Ki = 10.0 nM 8.00
CHEMBL4552310 Ki = 12.0 nM 7.92
CHEMBL4470026 Ki = 20.0 nM 7.70
CHEMBL4473140 Ki = 22.0 nM 7.66
CHEMBL4542463 Ki = 22.0 nM 7.66
CHEMBL4593649 Ki = 24.0 nM 7.62
CHEMBL4522276 Ki = 30.0 nM 7.52
CHEMBL4447403 Ki = 32.0 nM 7.50
CHEMBL4472438 Ki = 33.0 nM 7.48
CHEMBL4582326 Ki = 39.0 nM 7.41
CHEMBL4561238 Ki = 44.0 nM 7.36
CHEMBL4534571 Ki = 59.0 nM 7.23