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Assay Detail

CHEMBL4602786

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

Binding
Inhibition of human CK1delta
20
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Casein kinase I isoform delta (CHEMBL2828)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Roy SM, Minasov G, Arancio O, Chico LW, Van Eldik LJ, Anderson WF, Pelletier JC, Watterson DM.
J Med Chem (2019) 62 : 5298 -5311
PubMed 30978288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.94 7.30
Ki 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4632881 2 7.40
CHEMBL4639028 1 7.30
CHEMBL4639555 1 6.96
CHEMBL4648747 1 6.60
CHEMBL4635980 1 6.50
CHEMBL4642101 1 6.47
CHEMBL4645737 1 6.15
CHEMBL4647072 1 5.70
CHEMBL4129018 MW-150 2.0 1 5.58
CHEMBL4639995 1 5.50
CHEMBL4643993 1 5.28
CHEMBL4643246 1 5.23
CHEMBL4648060 1 5.18
CHEMBL4635988 1 5.04
CHEMBL4643060 1 5.00
CHEMBL4642456 1 -
CHEMBL4640881 1 -
CHEMBL4646628 1 -
CHEMBL10 SB-203580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4632881 Ki = 40.0 nM 7.40
CHEMBL4639028 IC50 = 50.0 nM 7.30
CHEMBL4639555 IC50 = 110.0 nM 6.96
CHEMBL4632881 IC50 = 230.0 nM 6.64
CHEMBL4648747 IC50 = 250.0 nM 6.60
CHEMBL4635980 IC50 = 320.0 nM 6.50
CHEMBL4642101 IC50 = 340.0 nM 6.47
CHEMBL4645737 IC50 = 710.0 nM 6.15
CHEMBL4647072 IC50 = 2020.0 nM 5.70
CHEMBL4129018 MW-150 IC50 = 2610.0 nM 5.58
CHEMBL4639995 IC50 = 3190.0 nM 5.50
CHEMBL4643993 IC50 = 5210.0 nM 5.28
CHEMBL4643246 IC50 = 5830.0 nM 5.23
CHEMBL4648060 IC50 = 6650.0 nM 5.18
CHEMBL4635988 IC50 = 9130.0 nM 5.04
CHEMBL4643060 IC50 = 10020.0 nM 5.00
CHEMBL4642456 IC50 > 10000.0 nM -
CHEMBL4640881 IC50 > 10000.0 nM -
CHEMBL4646628 IC50 > 10000.0 nM -
CHEMBL10 SB-203580 IC50 < 1000.0 nM -