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

CHEMBL5241009

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

Binding
Inhibition of tau phosphorylation (unknown origin)
ChEMBL ↗
68
Total Activities
68
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

Microtubule-associated protein tau (CHEMBL1293224) ↗
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 68 6.98 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5278104 — — 1 9.40
CHEMBL5291181 — — 1 8.77
CHEMBL5284020 — — 1 8.72
CHEMBL5290966 — — 1 8.70
CHEMBL5268011 — — 1 8.55
CHEMBL5282887 — — 1 8.30
CHEMBL5282113 — — 1 7.92
CHEMBL5274489 — — 1 7.82
CHEMBL5281590 — — 1 7.75
CHEMBL5268820 — — 1 7.72
CHEMBL5289779 — — 1 7.64
CHEMBL5288950 — — 1 7.64
CHEMBL5282618 — — 1 7.60
CHEMBL5272041 — — 1 7.60
CHEMBL5286043 — — 1 7.52
CHEMBL5276076 — — 1 7.51
CHEMBL5283410 — — 1 7.46
CHEMBL5290846 — — 1 7.43
CHEMBL5266570 — — 1 7.39
CHEMBL5287592 — — 1 7.37
CHEMBL5277764 — — 1 7.32
CHEMBL5272115 — — 1 7.30
CHEMBL5271077 — — 1 7.16
CHEMBL5280118 — — 1 7.16
CHEMBL5270059 — — 1 7.14
CHEMBL5276749 — — 1 7.14
CHEMBL5290181 — — 1 7.12
CHEMBL5265899 — — 1 7.10
CHEMBL5285048 — — 1 7.10
CHEMBL5280453 — — 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5278104 — IC50 = 0.4 nM 9.40
CHEMBL5291181 — IC50 = 1.7 nM 8.77
CHEMBL5284020 — IC50 = 1.9 nM 8.72
CHEMBL5290966 — IC50 = 2.0 nM 8.70
CHEMBL5268011 — IC50 = 2.8 nM 8.55
CHEMBL5282887 — IC50 = 5.0 nM 8.30
CHEMBL5282113 — IC50 = 12.0 nM 7.92
CHEMBL5274489 — IC50 = 15.0 nM 7.82
CHEMBL5281590 — IC50 = 18.0 nM 7.75
CHEMBL5268820 — IC50 = 19.0 nM 7.72
CHEMBL5289779 — IC50 = 23.0 nM 7.64
CHEMBL5288950 — IC50 = 23.0 nM 7.64
CHEMBL5272041 — IC50 = 25.0 nM 7.60
CHEMBL5282618 — IC50 = 25.0 nM 7.60
CHEMBL5286043 — IC50 = 30.0 nM 7.52
CHEMBL5276076 — IC50 = 31.0 nM 7.51
CHEMBL5283410 — IC50 = 35.0 nM 7.46
CHEMBL5290846 — IC50 = 37.0 nM 7.43
CHEMBL5266570 — IC50 = 41.0 nM 7.39
CHEMBL5287592 — IC50 = 43.0 nM 7.37
CHEMBL5277764 — IC50 = 48.0 nM 7.32
CHEMBL5272115 — IC50 = 50.0 nM 7.30
CHEMBL5271077 — IC50 = 70.0 nM 7.16
CHEMBL5280118 — IC50 = 69.0 nM 7.16
CHEMBL5276749 — IC50 = 72.0 nM 7.14
CHEMBL5270059 — IC50 = 73.0 nM 7.14
CHEMBL5290181 — IC50 = 76.0 nM 7.12
CHEMBL5265899 — IC50 = 80.0 nM 7.10
CHEMBL5285048 — IC50 = 79.0 nM 7.10
CHEMBL5280453 — IC50 = 85.0 nM 7.07
CHEMBL5272462 — IC50 = 94.0 nM 7.03
CHEMBL5273399 — IC50 = 94.0 nM 7.03
CHEMBL5291257 — IC50 = 100.0 nM 7.00
CHEMBL5287772 — IC50 = 99.0 nM 7.00
CHEMBL5273034 — IC50 = 110.0 nM 6.96
CHEMBL5276314 — IC50 = 120.0 nM 6.92
CHEMBL5276840 — IC50 = 120.0 nM 6.92
CHEMBL5282635 — IC50 = 120.0 nM 6.92
CHEMBL5269369 — IC50 = 130.0 nM 6.89
CHEMBL5281994 — IC50 = 150.0 nM 6.82
CHEMBL5276201 — IC50 = 150.0 nM 6.82
CHEMBL5266186 — IC50 = 160.0 nM 6.80
CHEMBL5271607 — IC50 = 160.0 nM 6.80
CHEMBL5272651 — IC50 = 170.0 nM 6.77
CHEMBL5289493 — IC50 = 180.0 nM 6.75
CHEMBL5286727 — IC50 = 190.0 nM 6.72
CHEMBL5272013 — IC50 = 220.0 nM 6.66
CHEMBL5267564 — IC50 = 260.0 nM 6.58
CHEMBL5284249 — IC50 = 300.0 nM 6.52
CHEMBL5285396 — IC50 = 320.0 nM 6.50