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Assay Detail

CHEMBL4031112

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

Binding
Inhibition of Atrovastatin-PEG3-FITC binding to PDEdelta (unknown origin) incubated for 60 mins by fluorescence anisotropy assay
19
Total Activities
17
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

Structural Biology-Inspired Discovery of Novel KRAS-PDEδ Inhibitors.
Jiang Y, Zhuang C, Chen L, Lu J, Dong G, Miao Z, Zhang W, Li J, Sheng C.
J Med Chem (2017) 60 : 9400 -9406
PubMed 28929751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 7.83 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061005 3 9.22
CHEMBL1387422 1 8.66
CHEMBL4090695 1 8.64
CHEMBL4061982 1 8.40
CHEMBL4082888 1 8.40
CHEMBL4090022 1 8.10
CHEMBL4091313 1 8.05
CHEMBL4092911 1 7.92
CHEMBL4069561 1 7.82
CHEMBL4072582 1 7.80
CHEMBL4060010 1 7.66
CHEMBL3286929 1 7.62
CHEMBL4080394 1 7.48
CHEMBL4073704 1 7.24
CHEMBL4084687 1 7.12
CHEMBL4083592 1 6.64
CHEMBL4098417 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061005 Kd = 0.6 nM 9.22
CHEMBL4061005 Kd = 2.0 nM 8.70
CHEMBL1387422 Kd = 2.2 nM 8.66
CHEMBL4090695 Kd = 2.3 nM 8.64
CHEMBL4061982 Kd = 4.0 nM 8.40
CHEMBL4082888 Kd = 4.0 nM 8.40
CHEMBL4090022 Kd = 8.0 nM 8.10
CHEMBL4091313 Kd = 9.0 nM 8.05
CHEMBL4092911 Kd = 12.0 nM 7.92
CHEMBL4069561 Kd = 15.0 nM 7.82
CHEMBL4072582 Kd = 16.0 nM 7.80
CHEMBL4060010 Kd = 22.0 nM 7.66
CHEMBL3286929 Kd = 24.0 nM 7.62
CHEMBL4080394 Kd = 33.0 nM 7.48
CHEMBL4061005 Kd = 37.0 nM 7.43
CHEMBL4073704 Kd = 57.8 nM 7.24
CHEMBL4084687 Kd = 76.0 nM 7.12
CHEMBL4083592 Kd = 227.0 nM 6.64
CHEMBL4098417 Kd = 1119.0 nM 5.95