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Assay Detail

CHEMBL932635

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

Binding
Inhibition of PKBbeta recombinant by radiometric filter binding assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

RAC-beta serine/threonine-protein kinase (CHEMBL2431)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I.
J Med Chem (2008) 51 : 2147 -2157
PubMed 18345609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.83 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409503 1 8.52
CHEMBL260000 1 8.30
CHEMBL263664 1 8.22
CHEMBL407504 1 8.15
CHEMBL259998 1 8.15
CHEMBL406863 1 8.10
CHEMBL260577 1 7.92
CHEMBL260358 1 7.80
CHEMBL228133 1 7.70
CHEMBL259999 1 7.60
CHEMBL405384 1 7.60
CHEMBL260463 1 7.60
CHEMBL261034 1 7.15
CHEMBL259141 1 6.75
CHEMBL261247 1 6.61
CHEMBL261260 1 6.57
CHEMBL259356 1 6.54
CHEMBL104264 1 6.23
CHEMBL261249 1 6.11
CHEMBL265451 1 6.08
CHEMBL264965 1 6.06
CHEMBL265193 1 6.04
CHEMBL376388 1 5.16
CHEMBL264667 1 4.39
CHEMBL264666 1 4.23
CHEMBL265194 1 3.96
CHEMBL389685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409503 IC50 = 3.0 nM 8.52
CHEMBL260000 IC50 = 5.0 nM 8.30
CHEMBL263664 IC50 = 6.0 nM 8.22
CHEMBL407504 IC50 = 7.0 nM 8.15
CHEMBL259998 IC50 = 7.0 nM 8.15
CHEMBL406863 IC50 = 8.0 nM 8.10
CHEMBL260577 IC50 = 12.0 nM 7.92
CHEMBL260358 IC50 = 16.0 nM 7.80
CHEMBL228133 IC50 = 20.0 nM 7.70
CHEMBL259999 IC50 = 25.0 nM 7.60
CHEMBL405384 IC50 = 25.0 nM 7.60
CHEMBL260463 IC50 = 25.0 nM 7.60
CHEMBL261034 IC50 = 71.0 nM 7.15
CHEMBL259141 IC50 = 180.0 nM 6.75
CHEMBL261247 IC50 = 246.0 nM 6.61
CHEMBL261260 IC50 = 270.0 nM 6.57
CHEMBL259356 IC50 = 290.0 nM 6.54
CHEMBL104264 IC50 = 590.0 nM 6.23
CHEMBL261249 IC50 = 770.0 nM 6.11
CHEMBL265451 IC50 = 830.0 nM 6.08
CHEMBL264965 IC50 = 880.0 nM 6.06
CHEMBL265193 IC50 = 920.0 nM 6.04
CHEMBL376388 IC50 = 6900.0 nM 5.16
CHEMBL264667 IC50 = 41000.0 nM 4.39
CHEMBL264666 IC50 = 59000.0 nM 4.23
CHEMBL265194 IC50 = 110000.0 nM 3.96
CHEMBL389685 IC50 > 100000.0 nM -