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Assay Detail

CHEMBL684359

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Binding
Ability to inhibit 50% glycogen synthase kinase-3 beta of recombinant human, expressed as log of concentration
ChEMBL ↗
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors.
Peat AJ, Boucheron JA, Dickerson SH, Garrido D, Mills W, Peckham J, Preugschat F, Smalley T, Schweiker SL, Wilson JR, Wang TY, Zhou HQ, Thomson SA.
Bioorg Med Chem Lett (2004) 14 : 2121 -2125
PubMed 15080992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 7.25 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 — 1 8.60
CHEMBL303630 — — 1 8.60
CHEMBL308454 — — 1 8.50
CHEMBL66791 — — 1 8.40
CHEMBL66453 — — 1 8.40
CHEMBL63915 — — 1 8.30
CHEMBL309152 — — 1 8.30
CHEMBL303321 — — 1 8.20
CHEMBL306865 GW784752X — 1 8.20
CHEMBL65884 GW817396X — 1 8.10
CHEMBL65987 — — 1 8.10
CHEMBL69757 GW817394X — 1 8.10
CHEMBL69588 — — 1 8.00
CHEMBL308455 — — 1 8.00
CHEMBL418690 — — 1 8.00
CHEMBL66170 — — 1 8.00
CHEMBL68450 — — 1 8.00
CHEMBL308430 — — 1 7.90
CHEMBL66900 — — 1 7.90
CHEMBL304172 — — 1 7.90
CHEMBL67374 — — 1 7.80
CHEMBL303433 — — 1 7.80
CHEMBL67799 — — 1 7.80
CHEMBL66543 — — 1 7.80
CHEMBL305477 GW829874X — 1 7.60
CHEMBL302048 — — 1 7.50
CHEMBL66910 — — 1 7.50
CHEMBL63414 — — 1 7.50
CHEMBL65988 — — 1 7.50
CHEMBL68397 — — 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 IC50 = 2.512 nM 8.60
CHEMBL303630 — IC50 = 2.512 nM 8.60
CHEMBL308454 — IC50 = 3.162 nM 8.50
CHEMBL66791 — IC50 = 3.981 nM 8.40
CHEMBL66453 — IC50 = 3.981 nM 8.40
CHEMBL63915 — IC50 = 5.012 nM 8.30
CHEMBL309152 — IC50 = 5.012 nM 8.30
CHEMBL303321 — IC50 = 6.31 nM 8.20
CHEMBL306865 GW784752X IC50 = 6.31 nM 8.20
CHEMBL65884 GW817396X IC50 = 7.943 nM 8.10
CHEMBL65987 — IC50 = 7.943 nM 8.10
CHEMBL69757 GW817394X IC50 = 7.943 nM 8.10
CHEMBL66170 — IC50 = 10.0 nM 8.00
CHEMBL308455 — IC50 = 10.0 nM 8.00
CHEMBL69588 — IC50 = 10.0 nM 8.00
CHEMBL418690 — IC50 = 10.0 nM 8.00
CHEMBL68450 — IC50 = 10.0 nM 8.00
CHEMBL308430 — IC50 = 12.59 nM 7.90
CHEMBL66900 — IC50 = 12.59 nM 7.90
CHEMBL304172 — IC50 = 12.59 nM 7.90
CHEMBL67374 — IC50 = 15.85 nM 7.80
CHEMBL303433 — IC50 = 15.85 nM 7.80
CHEMBL67799 — IC50 = 15.85 nM 7.80
CHEMBL66543 — IC50 = 15.85 nM 7.80
CHEMBL305477 GW829874X IC50 = 25.12 nM 7.60
CHEMBL302048 — IC50 = 31.62 nM 7.50
CHEMBL65988 — IC50 = 31.62 nM 7.50
CHEMBL66910 — IC50 = 31.62 nM 7.50
CHEMBL63414 — IC50 = 31.62 nM 7.50
CHEMBL68397 — IC50 = 39.81 nM 7.40
CHEMBL302490 — IC50 = 39.81 nM 7.40
CHEMBL302969 — IC50 = 63.1 nM 7.20
CHEMBL66510 — IC50 = 100.0 nM 7.00
CHEMBL63803 — IC50 = 100.0 nM 7.00
CHEMBL63727 — IC50 = 100.0 nM 7.00
CHEMBL307311 — IC50 = 125.89 nM 6.90
CHEMBL67733 — IC50 = 158.49 nM 6.80
CHEMBL63348 — IC50 = 158.49 nM 6.80
CHEMBL294592 — IC50 = 158.49 nM 6.80
CHEMBL291425 — IC50 = 158.49 nM 6.80
CHEMBL67310 — IC50 = 251.19 nM 6.60
CHEMBL306692 — IC50 = 316.23 nM 6.50
CHEMBL67562 — IC50 = 316.23 nM 6.50
CHEMBL410319 — IC50 = 630.96 nM 6.20
CHEMBL68242 — IC50 = 1000.0 nM 6.00
CHEMBL304339 — IC50 = 1258.93 nM 5.90
CHEMBL69526 — IC50 = 1995.26 nM 5.70
CHEMBL63728 GW644007X IC50 = 2511.89 nM 5.60
CHEMBL63595 — IC50 = 2511.89 nM 5.60
CHEMBL294595 — IC50 = 2511.89 nM 5.60