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Assay Detail

CHEMBL4121733

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Binding
Inhibition of PI3Kgamma (unknown origin)
12
Total Activities
12
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

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 12 5.90 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127319 1 7.90
CHEMBL4126566 1 7.00
CHEMBL4129590 1 5.80
CHEMBL4127640 1 5.60
CHEMBL4126300 1 5.40
CHEMBL4126413 1 5.20
CHEMBL4129219 1 5.20
CHEMBL4128625 1 5.10
CHEMBL4129843 1 -
CHEMBL4129991 1 -
CHEMBL4129040 1 -
CHEMBL4127797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127319 IC50 = 12.59 nM 7.90
CHEMBL4126566 IC50 = 100.0 nM 7.00
CHEMBL4129590 IC50 = 1584.89 nM 5.80
CHEMBL4127640 IC50 = 2511.89 nM 5.60
CHEMBL4126300 IC50 = 3981.07 nM 5.40
CHEMBL4126413 IC50 = 6309.57 nM 5.20
CHEMBL4129219 IC50 = 6309.57 nM 5.20
CHEMBL4128625 IC50 = 7943.28 nM 5.10
CHEMBL4129843 IC50 > 10000.0 nM -
CHEMBL4129991 IC50 > 10000.0 nM -
CHEMBL4129040 IC50 > 10000.0 nM -
CHEMBL4127797 IC50 > 10000.0 nM -