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Assay Detail

CHEMBL5046564

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

Binding
Inhibition of recombinant human GSK-3-beta using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr in presence of ATP by ADP Glo kinase assay
ChEMBL ↗
48
Total Activities
25
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

Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors.
Andreev S, Pantsar T, Tesch R, Kahlke N, El-Gokha A, Ansideri F, Grätz L, Romasco J, Sita G, Geibel C, Lämmerhofer M, Tarozzi A, Knapp S, Laufer SA, Koch P.
J Med Chem (2022) 65 : 1283 -1301
PubMed 34213342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.28 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5077814 — — 2 8.70
CHEMBL5089934 — — 2 8.22
CHEMBL5084461 — — 2 7.64
CHEMBL5088263 — — 2 7.20
CHEMBL5071096 — — 2 6.90
CHEMBL5074629 — — 2 6.90
CHEMBL5089614 — — 2 6.50
CHEMBL5086422 — — 2 6.41
CHEMBL5081810 — — 2 6.40
CHEMBL5089053 — — 2 6.32
CHEMBL5081917 — — 2 6.31
CHEMBL5084003 — — 2 6.15
CHEMBL5087421 — — 2 6.12
CHEMBL5078490 — — 2 6.01
CHEMBL5076549 — — 2 5.92
CHEMBL5082566 — — 2 5.90
CHEMBL5075604 — — 2 5.60
CHEMBL5085025 — — 2 5.42
CHEMBL5071724 — — 2 5.30
CHEMBL5093829 — — 2 5.30
CHEMBL5074611 — — 2 5.21
CHEMBL5079159 — — 2 5.10
CHEMBL5076997 — — 2 5.10
CHEMBL5078899 — — 1 -
CHEMBL5088570 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5077814 — IC50 = 1.995 nM 8.70
CHEMBL5077814 — IC50 = 2.0 nM 8.70
CHEMBL5089934 — IC50 = 6.0 nM 8.22
CHEMBL5089934 — IC50 = 6.31 nM 8.20
CHEMBL5084461 — IC50 = 23.0 nM 7.64
CHEMBL5084461 — IC50 = 25.12 nM 7.60
CHEMBL5088263 — IC50 = 63.1 nM 7.20
CHEMBL5088263 — IC50 = 66.0 nM 7.18
CHEMBL5071096 — IC50 = 125.89 nM 6.90
CHEMBL5074629 — IC50 = 125.89 nM 6.90
CHEMBL5074629 — IC50 = 130.0 nM 6.89
CHEMBL5071096 — IC50 = 132.0 nM 6.88
CHEMBL5089614 — IC50 = 316.23 nM 6.50
CHEMBL5089614 — IC50 = 319.0 nM 6.50
CHEMBL5086422 — IC50 = 388.0 nM 6.41
CHEMBL5081810 — IC50 = 398.11 nM 6.40
CHEMBL5086422 — IC50 = 398.11 nM 6.40
CHEMBL5081810 — IC50 = 408.0 nM 6.39
CHEMBL5089053 — IC50 = 480.0 nM 6.32
CHEMBL5081917 — IC50 = 489.0 nM 6.31
CHEMBL5081917 — IC50 = 501.19 nM 6.30
CHEMBL5089053 — IC50 = 501.19 nM 6.30
CHEMBL5084003 — IC50 = 712.0 nM 6.15
CHEMBL5087421 — IC50 = 764.0 nM 6.12
CHEMBL5087421 — IC50 = 794.33 nM 6.10
CHEMBL5084003 — IC50 = 794.33 nM 6.10
CHEMBL5078490 — IC50 = 973.0 nM 6.01
CHEMBL5078490 — IC50 = 1000.0 nM 6.00
CHEMBL5076549 — IC50 = 1204.0 nM 5.92
CHEMBL5082566 — IC50 = 1258.93 nM 5.90
CHEMBL5076549 — IC50 = 1258.93 nM 5.90
CHEMBL5082566 — IC50 = 1382.0 nM 5.86
CHEMBL5075604 — IC50 = 2511.89 nM 5.60
CHEMBL5075604 — IC50 = 2668.0 nM 5.57
CHEMBL5085025 — IC50 = 3811.0 nM 5.42
CHEMBL5085025 — IC50 = 3981.07 nM 5.40
CHEMBL5071724 — IC50 = 5011.87 nM 5.30
CHEMBL5093829 — IC50 = 5011.87 nM 5.30
CHEMBL5093829 — IC50 = 5112.0 nM 5.29
CHEMBL5071724 — IC50 = 5299.0 nM 5.28
CHEMBL5074611 — IC50 = 6096.0 nM 5.21
CHEMBL5074611 — IC50 = 6309.57 nM 5.20
CHEMBL5079159 — IC50 = 7943.28 nM 5.10
CHEMBL5076997 — IC50 = 7943.28 nM 5.10
CHEMBL5076997 — IC50 = 8042.0 nM 5.09
CHEMBL5079159 — IC50 = 8690.0 nM 5.06
CHEMBL5088570 — IC50 > 10000.0 nM -
CHEMBL5078899 — IC50 > 10000.0 nM -