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Assay Detail

CHEMBL5343395

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

Binding
Displacement of FL-KRREILSRRP[ps]ERYR-NH2 from human recombinant N-terminal His6-tagged GSK-3-beta (14 to 306 residues) H355L mutant expressed in baculovirus-infected Sf21 cells incubated for 20 hrs by fluorescence based analysis
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycogen synthase kinase-3 beta (CHEMBL262) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Hartz RA, Ahuja VT, Luo G, Chen L, Sivaprakasam P, Xiao H, Krause CM, Clarke WJ, Xu S, Tokarski JS, Kish K, Lewis H, Szapiel N, Ravirala R, Mutalik S, Nakmode D, Shah D, Burton CR, Macor JE, Dubowchik GM.
J Med Chem (2023) 66 : 7534 -7552
PubMed 37235865 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.93 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5409061 — — 1 10.15
CHEMBL5404581 — — 1 9.82
CHEMBL5418606 — — 1 9.74
CHEMBL5416472 — — 1 9.70
CHEMBL5437994 — — 1 9.70
CHEMBL5440672 — — 1 9.62
CHEMBL5407971 — — 1 9.60
CHEMBL5414726 — — 1 9.60
CHEMBL5422776 — — 1 9.55
CHEMBL5436595 — — 1 9.51
CHEMBL5419652 — — 1 9.46
CHEMBL5404070 — — 1 9.37
CHEMBL5424348 — — 1 9.37
CHEMBL5422112 — — 1 9.35
CHEMBL5438689 — — 1 9.35
CHEMBL5435368 — — 1 9.35
CHEMBL5414551 — — 1 9.31
CHEMBL5402829 — — 1 9.25
CHEMBL5428013 — — 1 9.13
CHEMBL5415012 — — 1 9.05
CHEMBL5413819 — — 1 9.05
CHEMBL5417065 — — 1 8.96
CHEMBL5432510 — — 1 8.96
CHEMBL5401931 — — 1 8.96
CHEMBL5410129 — — 1 8.92
CHEMBL5433893 — — 1 8.74
CHEMBL5420646 — — 1 8.70
CHEMBL5429353 — — 1 8.70
CHEMBL5431425 — — 1 8.68
CHEMBL5428489 — — 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5409061 — IC50 = 0.07 nM 10.15
CHEMBL5404581 — IC50 = 0.15 nM 9.82
CHEMBL5418606 — IC50 = 0.18 nM 9.74
CHEMBL5416472 — IC50 = 0.2 nM 9.70
CHEMBL5437994 — IC50 = 0.2 nM 9.70
CHEMBL5440672 — IC50 = 0.24 nM 9.62
CHEMBL5407971 — IC50 = 0.25 nM 9.60
CHEMBL5414726 — IC50 = 0.25 nM 9.60
CHEMBL5422776 — IC50 = 0.28 nM 9.55
CHEMBL5436595 — IC50 = 0.31 nM 9.51
CHEMBL5419652 — IC50 = 0.35 nM 9.46
CHEMBL5404070 — IC50 = 0.43 nM 9.37
CHEMBL5424348 — IC50 = 0.43 nM 9.37
CHEMBL5435368 — IC50 = 0.45 nM 9.35
CHEMBL5438689 — IC50 = 0.45 nM 9.35
CHEMBL5422112 — IC50 = 0.45 nM 9.35
CHEMBL5414551 — IC50 = 0.49 nM 9.31
CHEMBL5402829 — IC50 = 0.56 nM 9.25
CHEMBL5428013 — IC50 = 0.74 nM 9.13
CHEMBL5413819 — IC50 = 0.89 nM 9.05
CHEMBL5415012 — IC50 = 0.9 nM 9.05
CHEMBL5417065 — IC50 = 1.1 nM 8.96
CHEMBL5432510 — IC50 = 1.1 nM 8.96
CHEMBL5401931 — IC50 = 1.1 nM 8.96
CHEMBL5410129 — IC50 = 1.2 nM 8.92
CHEMBL5433893 — IC50 = 1.8 nM 8.74
CHEMBL5420646 — IC50 = 2.0 nM 8.70
CHEMBL5429353 — IC50 = 2.0 nM 8.70
CHEMBL5431425 — IC50 = 2.1 nM 8.68
CHEMBL5428489 — IC50 = 3.8 nM 8.42
CHEMBL5434336 — IC50 = 3.9 nM 8.41
CHEMBL5278465 — IC50 = 5.9 nM 8.23
CHEMBL5409415 — IC50 = 13.0 nM 7.89
CHEMBL5434002 — IC50 = 20.0 nM 7.70
CHEMBL5430845 — IC50 = 30.0 nM 7.52
CHEMBL102714 SB-216763 IC50 = 34.0 nM 7.47
CHEMBL1232916 — IC50 = 53.0 nM 7.28
CHEMBL5408273 — IC50 = 260.0 nM 6.58
CHEMBL5430407 — IC50 > 2000.0 nM -
CHEMBL5397608 — IC50 > 2000.0 nM -