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Assay Detail

CHEMBL5241008

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

Binding
Inhibition of GSK-3beta (unknown origin) incubated for 1 hr by HTRF assay
ChEMBL ↗
65
Total Activities
65
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

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

Publication

Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Luo G, Chen L, Jacutin-Porte S, Han Y, Burton CR, Xiao H, Krause CM, Cao Y, Liu N, Kish K, Lewis HA, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2023) 81 : 129143 -129143
PubMed 36669575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 8.54 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5290966 — — 1 10.22
CHEMBL5268011 — — 1 10.00
CHEMBL5278104 — — 1 9.82
CHEMBL5284020 — — 1 9.80
CHEMBL5282887 — — 1 9.72
CHEMBL5283410 — — 1 9.60
CHEMBL5291181 — — 1 9.43
CHEMBL5286043 — — 1 9.34
CHEMBL5282113 — — 1 9.31
CHEMBL5276076 — — 1 9.21
CHEMBL5271077 — — 1 9.14
CHEMBL5272041 — — 1 9.10
CHEMBL5290181 — — 1 9.07
CHEMBL5273034 — — 1 9.02
CHEMBL5281590 — — 1 9.00
CHEMBL5288950 — — 1 9.00
CHEMBL5273531 — — 1 9.00
CHEMBL5289779 — — 1 9.00
CHEMBL5286581 — — 1 8.92
CHEMBL5271607 — — 1 8.85
CHEMBL5289493 — — 1 8.85
CHEMBL5272115 — — 1 8.85
CHEMBL5290846 — — 1 8.77
CHEMBL5272651 — — 1 8.77
CHEMBL5266570 — — 1 8.74
CHEMBL5282635 — — 1 8.72
CHEMBL5280118 — — 1 8.68
CHEMBL5276749 — — 1 8.66
CHEMBL5287772 — — 1 8.64
CHEMBL5270059 — — 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5290966 — IC50 = 0.06 nM 10.22
CHEMBL5268011 — IC50 = 0.1 nM 10.00
CHEMBL5278104 — IC50 = 0.15 nM 9.82
CHEMBL5284020 — IC50 = 0.16 nM 9.80
CHEMBL5282887 — IC50 = 0.19 nM 9.72
CHEMBL5283410 — IC50 = 0.25 nM 9.60
CHEMBL5291181 — IC50 = 0.37 nM 9.43
CHEMBL5286043 — IC50 = 0.46 nM 9.34
CHEMBL5282113 — IC50 = 0.49 nM 9.31
CHEMBL5276076 — IC50 = 0.62 nM 9.21
CHEMBL5271077 — IC50 = 0.72 nM 9.14
CHEMBL5272041 — IC50 = 0.79 nM 9.10
CHEMBL5290181 — IC50 = 0.85 nM 9.07
CHEMBL5273034 — IC50 = 0.95 nM 9.02
CHEMBL5289779 — IC50 = 1.0 nM 9.00
CHEMBL5288950 — IC50 = 0.99 nM 9.00
CHEMBL5273531 — IC50 = 1.0 nM 9.00
CHEMBL5281590 — IC50 = 0.99 nM 9.00
CHEMBL5286581 — IC50 = 1.2 nM 8.92
CHEMBL5271607 — IC50 = 1.4 nM 8.85
CHEMBL5289493 — IC50 = 1.4 nM 8.85
CHEMBL5272115 — IC50 = 1.4 nM 8.85
CHEMBL5290846 — IC50 = 1.7 nM 8.77
CHEMBL5272651 — IC50 = 1.7 nM 8.77
CHEMBL5266570 — IC50 = 1.8 nM 8.74
CHEMBL5282635 — IC50 = 1.9 nM 8.72
CHEMBL5280118 — IC50 = 2.1 nM 8.68
CHEMBL5276749 — IC50 = 2.2 nM 8.66
CHEMBL5287772 — IC50 = 2.3 nM 8.64
CHEMBL5270059 — IC50 = 2.5 nM 8.60
CHEMBL5276314 — IC50 = 2.5 nM 8.60
CHEMBL5269369 — IC50 = 2.5 nM 8.60
CHEMBL5285048 — IC50 = 2.6 nM 8.59
CHEMBL5268820 — IC50 = 2.8 nM 8.55
CHEMBL5266186 — IC50 = 3.0 nM 8.52
CHEMBL5277764 — IC50 = 3.6 nM 8.44
CHEMBL5291257 — IC50 = 3.7 nM 8.43
CHEMBL5276201 — IC50 = 3.9 nM 8.41
CHEMBL5271312 — IC50 = 4.1 nM 8.39
CHEMBL5272462 — IC50 = 4.1 nM 8.39
CHEMBL5276840 — IC50 = 4.2 nM 8.38
CHEMBL5265899 — IC50 = 4.4 nM 8.36
CHEMBL5283804 — IC50 = 4.5 nM 8.35
CHEMBL5273399 — IC50 = 4.6 nM 8.34
CHEMBL5285396 — IC50 = 4.8 nM 8.32
CHEMBL5280453 — IC50 = 5.6 nM 8.25
CHEMBL5267564 — IC50 = 5.7 nM 8.24
CHEMBL5272358 — IC50 = 6.4 nM 8.19
CHEMBL5281994 — IC50 = 6.9 nM 8.16
CHEMBL5268992 — IC50 = 7.5 nM 8.12