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Assay Detail

CHEMBL4121734

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Binding
Inhibition of IKK1 (unknown origin)
20
Total Activities
20
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 20 6.63 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128114 1 7.50
CHEMBL4125774 1 7.10
CHEMBL4127140 1 7.10
CHEMBL4125907 1 7.10
CHEMBL4128939 1 7.00
CHEMBL4126740 1 6.90
CHEMBL4126095 1 6.90
CHEMBL4130310 1 6.90
CHEMBL4129362 1 6.80
CHEMBL4127977 1 6.80
CHEMBL4129791 1 6.80
CHEMBL4128717 1 6.80
CHEMBL4127479 1 6.70
CHEMBL4126511 1 5.60
CHEMBL4128577 1 5.60
CHEMBL4128459 1 5.60
CHEMBL4127330 1 5.50
CHEMBL4129941 1 -
CHEMBL4127076 1 -
CHEMBL4128540 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128114 IC50 = 31.62 nM 7.50
CHEMBL4125774 IC50 = 79.43 nM 7.10
CHEMBL4127140 IC50 = 79.43 nM 7.10
CHEMBL4125907 IC50 = 79.43 nM 7.10
CHEMBL4128939 IC50 = 100.0 nM 7.00
CHEMBL4126740 IC50 = 125.89 nM 6.90
CHEMBL4126095 IC50 = 125.89 nM 6.90
CHEMBL4130310 IC50 = 125.89 nM 6.90
CHEMBL4129362 IC50 = 158.49 nM 6.80
CHEMBL4127977 IC50 = 158.49 nM 6.80
CHEMBL4129791 IC50 = 158.49 nM 6.80
CHEMBL4128717 IC50 = 158.49 nM 6.80
CHEMBL4127479 IC50 = 199.53 nM 6.70
CHEMBL4126511 IC50 = 2511.89 nM 5.60
CHEMBL4128577 IC50 = 2511.89 nM 5.60
CHEMBL4128459 IC50 = 2511.89 nM 5.60
CHEMBL4127330 IC50 = 3162.28 nM 5.50
CHEMBL4129941 IC50 > 25118.86 nM -
CHEMBL4127076 IC50 > 31622.78 nM -
CHEMBL4128540 IC50 > 25118.86 nM -