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Assay Detail

CHEMBL4629886

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

Binding
Inhibition of recombinant human full-length His-tagged CAMK1D expressed in baculovirus expression system using autocamtide-2 as substrate preincubated for 15 mins followed by ATP addition and measured after 2 hrs by ADP-glo luminescence assay
15
Total Activities
15
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

Calcium/calmodulin-dependent protein kinase type 1D (CHEMBL5073)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity <i>in Vivo</i> Mouse Model.
Fromont C, Atzori A, Kaur D, Hashmi L, Greco G, Cabanillas A, Nguyen HV, Jones DH, Garzón M, Varela A, Stevenson B, Iacobini GP, Lenoir M, Rajesh S, Box C, Kumar J, Grant P, Novitskaya V, Morgan J, Sorrell FJ, Redondo C, Kramer A, Harris CJ, Leighton B, Vickers SP, Cheetham SC, Kenyon C, Grabowska AM, Overduin M, Berditchevski F, Weston CJ, Knapp S, Fischer PM, Butterworth S.
J Med Chem (2020) 63 : 6784 -6801
PubMed 32433887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.89 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635883 1 8.10
CHEMBL4633229 1 7.66
CHEMBL4632457 1 7.57
CHEMBL4640712 1 7.51
CHEMBL4644948 1 7.33
CHEMBL4640492 1 7.02
CHEMBL4640445 1 7.00
CHEMBL4634851 1 6.94
CHEMBL1835063 1 6.73
CHEMBL4632574 1 6.56
CHEMBL471901 1 6.37
CHEMBL4639597 1 6.34
CHEMBL4644912 1 6.31
CHEMBL4642539 1 6.07
CHEMBL4640950 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635883 IC50 = 8.0 nM 8.10
CHEMBL4633229 IC50 = 22.0 nM 7.66
CHEMBL4632457 IC50 = 27.0 nM 7.57
CHEMBL4640712 IC50 = 31.0 nM 7.51
CHEMBL4644948 IC50 = 47.0 nM 7.33
CHEMBL4640492 IC50 = 96.0 nM 7.02
CHEMBL4640445 IC50 = 101.0 nM 7.00
CHEMBL4634851 IC50 = 115.0 nM 6.94
CHEMBL1835063 IC50 = 186.0 nM 6.73
CHEMBL4632574 IC50 = 277.0 nM 6.56
CHEMBL471901 IC50 = 432.0 nM 6.37
CHEMBL4639597 IC50 = 455.0 nM 6.34
CHEMBL4644912 IC50 = 485.0 nM 6.31
CHEMBL4642539 IC50 = 851.0 nM 6.07
CHEMBL4640950 IC50 = 1350.0 nM 5.87