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

CHEMBL4121728

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

Binding
Inhibition of full-length human GST-tagged CAMKK2 using 5FAM-AKPKGNKDYHLQTCCGSLAYRRR-amide as substrate preincubated for 30 mins followed by substrate addition measured after 120 mins by fluorescence polarization assay
ChEMBL ↗
62
Total Activities
62
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 kinase 2 (CHEMBL5284) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.
Price DJ, Drewry DH, Schaller LT, Thompson BD, Reid PR, Maloney PR, Liang X, Banker P, Buckholz RG, Selley PK, McDonald OB, Smith JL, Shearer TW, Cox RF, Williams SP, Reid RA, Tacconi S, Faggioni F, Piubelli C, Sartori I, Tessari M, Wang TY.
Bioorg Med Chem Lett (2018) 28 : 1958 -1963
PubMed 29653895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 7.07 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126095 — — 1 8.80
CHEMBL4128577 — — 1 8.70
CHEMBL4129590 — — 1 8.70
CHEMBL4127245 — — 1 8.40
CHEMBL4128540 — — 1 8.20
CHEMBL4129219 — — 1 8.10
CHEMBL4126511 — — 1 8.10
CHEMBL558642 GSK-650394 — 1 8.10
CHEMBL4127977 — — 1 7.90
CHEMBL4127140 — — 1 7.90
CHEMBL4128459 — — 1 7.90
CHEMBL4126740 — — 1 7.90
CHEMBL4128114 — — 1 7.90
CHEMBL4128939 — — 1 7.90
CHEMBL4128717 — — 1 7.80
CHEMBL4127330 — — 1 7.80
CHEMBL4127064 — — 1 7.80
CHEMBL4129362 — — 1 7.70
CHEMBL4129791 — — 1 7.70
CHEMBL4129843 — — 1 7.70
CHEMBL550110 — — 1 7.70
CHEMBL4125907 — — 1 7.60
CHEMBL4126566 — — 1 7.60
CHEMBL4130310 — — 1 7.60
CHEMBL564555 — — 1 7.60
CHEMBL4125686 — — 1 7.50
CHEMBL4125774 — — 1 7.50
CHEMBL4127479 — — 1 7.50
CHEMBL4128483 — — 1 7.30
CHEMBL4126272 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126095 — IC50 = 1.585 nM 8.80
CHEMBL4128577 — IC50 = 1.995 nM 8.70
CHEMBL4129590 — IC50 = 1.995 nM 8.70
CHEMBL4127245 — IC50 = 3.981 nM 8.40
CHEMBL4128540 — IC50 = 6.31 nM 8.20
CHEMBL4129219 — IC50 = 7.943 nM 8.10
CHEMBL4126511 — IC50 = 7.943 nM 8.10
CHEMBL558642 GSK-650394 IC50 = 7.943 nM 8.10
CHEMBL4128939 — IC50 = 12.59 nM 7.90
CHEMBL4128114 — IC50 = 12.59 nM 7.90
CHEMBL4126740 — IC50 = 12.59 nM 7.90
CHEMBL4128459 — IC50 = 12.59 nM 7.90
CHEMBL4127140 — IC50 = 12.59 nM 7.90
CHEMBL4127977 — IC50 = 12.59 nM 7.90
CHEMBL4127064 — IC50 = 15.85 nM 7.80
CHEMBL4128717 — IC50 = 15.85 nM 7.80
CHEMBL4127330 — IC50 = 15.85 nM 7.80
CHEMBL4129362 — IC50 = 19.95 nM 7.70
CHEMBL4129791 — IC50 = 19.95 nM 7.70
CHEMBL4129843 — IC50 = 19.95 nM 7.70
CHEMBL550110 — IC50 = 19.95 nM 7.70
CHEMBL4125907 — IC50 = 25.12 nM 7.60
CHEMBL4126566 — IC50 = 25.12 nM 7.60
CHEMBL4130310 — IC50 = 25.12 nM 7.60
CHEMBL564555 — IC50 = 25.12 nM 7.60
CHEMBL4125686 — IC50 = 31.62 nM 7.50
CHEMBL4127479 — IC50 = 31.62 nM 7.50
CHEMBL4125774 — IC50 = 31.62 nM 7.50
CHEMBL4128483 — IC50 = 50.12 nM 7.30
CHEMBL4126272 — IC50 = 50.12 nM 7.30
CHEMBL4127319 — IC50 = 100.0 nM 7.00
CHEMBL4130255 — IC50 = 100.0 nM 7.00
CHEMBL4128950 — IC50 = 125.89 nM 6.90
CHEMBL546682 — IC50 = 125.89 nM 6.90
CHEMBL4127706 — IC50 = 199.53 nM 6.70
CHEMBL550795 — IC50 = 199.53 nM 6.70
CHEMBL4126332 — IC50 = 199.53 nM 6.70
CHEMBL4128625 — IC50 = 251.19 nM 6.60
CHEMBL4127076 — IC50 = 251.19 nM 6.60
CHEMBL4127797 — IC50 = 316.23 nM 6.50
CHEMBL4129941 — IC50 = 398.11 nM 6.40
CHEMBL4126920 — IC50 = 398.11 nM 6.40
CHEMBL4129709 — IC50 = 398.11 nM 6.40
CHEMBL4129991 — IC50 = 501.19 nM 6.30
CHEMBL4128151 — IC50 = 630.96 nM 6.20
CHEMBL4129130 — IC50 = 794.33 nM 6.10
CHEMBL564824 — IC50 = 1258.93 nM 5.90
CHEMBL4129040 — IC50 = 1258.93 nM 5.90
CHEMBL4126300 — IC50 = 1584.89 nM 5.80
CHEMBL4127557 — IC50 = 1584.89 nM 5.80