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Assay Detail

CHEMBL3382244

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

Binding
Binding affinity to DRAK2 (unknown origin) ATP site
45
Total Activities
45
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

Serine/threonine-protein kinase 17B (CHEMBL3980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach.
Gao LJ, Kovackova S, Sála M, Ramadori AT, De Jonghe S, Herdewijn P.
J Med Chem (2014) 57 : 7624 -7643
PubMed 25178155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 45 6.16 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3334979 1 8.05
CHEMBL3334980 1 7.57
CHEMBL3334981 1 7.48
CHEMBL3334988 1 6.75
CHEMBL3334978 1 6.29
CHEMBL3334963 1 6.28
CHEMBL3334946 1 6.18
CHEMBL3334983 1 6.02
CHEMBL3334961 1 5.80
CHEMBL3334959 1 5.80
CHEMBL3334955 1 5.80
CHEMBL3334958 1 5.72
CHEMBL3334945 1 5.70
CHEMBL3334962 1 5.66
CHEMBL3334948 1 5.64
CHEMBL3334982 1 5.57
CHEMBL3334949 1 5.50
CHEMBL3334970 1 5.14
CHEMBL3334975 1 -
CHEMBL3334967 1 -
CHEMBL3334976 1 -
CHEMBL3334977 1 -
CHEMBL3334960 1 -
CHEMBL3334964 1 -
CHEMBL3334965 1 -
CHEMBL3334966 1 -
CHEMBL3334984 1 -
CHEMBL3334985 1 -
CHEMBL3334986 1 -
CHEMBL3334987 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3334979 Kd = 9.0 nM 8.05
CHEMBL3334980 Kd = 27.0 nM 7.57
CHEMBL3334981 Kd = 33.0 nM 7.48
CHEMBL3334988 Kd = 180.0 nM 6.75
CHEMBL3334978 Kd = 510.0 nM 6.29
CHEMBL3334963 Kd = 530.0 nM 6.28
CHEMBL3334946 Kd = 660.0 nM 6.18
CHEMBL3334983 Kd = 960.0 nM 6.02
CHEMBL3334961 Kd = 1600.0 nM 5.80
CHEMBL3334959 Kd = 1600.0 nM 5.80
CHEMBL3334955 Kd = 1600.0 nM 5.80
CHEMBL3334958 Kd = 1900.0 nM 5.72
CHEMBL3334945 Kd = 2000.0 nM 5.70
CHEMBL3334962 Kd = 2200.0 nM 5.66
CHEMBL3334948 Kd = 2300.0 nM 5.64
CHEMBL3334982 Kd = 2700.0 nM 5.57
CHEMBL3334949 Kd = 3200.0 nM 5.50
CHEMBL3334970 Kd = 7200.0 nM 5.14
CHEMBL3334950 Kd - -
CHEMBL3334951 Kd - -
CHEMBL3334952 Kd - -
CHEMBL3334953 Kd - -
CHEMBL3334954 Kd - -
CHEMBL3334947 Kd - -
CHEMBL3334956 Kd - -
CHEMBL3334957 Kd - -
CHEMBL3334968 Kd - -
CHEMBL3334969 Kd - -
CHEMBL3334505 Kd - -
CHEMBL3334971 Kd - -
CHEMBL3334972 Kd - -
CHEMBL3334973 Kd - -
CHEMBL3334974 Kd - -
CHEMBL3334987 Kd - -
CHEMBL3334986 Kd - -
CHEMBL3334985 Kd - -
CHEMBL3334984 Kd - -
CHEMBL3334966 Kd - -
CHEMBL3334965 Kd - -
CHEMBL3334964 Kd - -
CHEMBL3334960 Kd - -
CHEMBL3334977 Kd - -
CHEMBL3334976 Kd - -
CHEMBL3334967 Kd - -
CHEMBL3334975 Kd - -