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Assay Detail

CHEMBL5540171

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

Binding
Inhibition of KRAS G12D mutant (unknown origin) preincubated for 15 mins followed by SOS1/EDA-GTP-DY-647P1 addition measured after 30 mins by HTRF assay
2
Total Activities
2
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

GTPase KRas (CHEMBL2189121)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRAS<sup>G12D</sup>.
Zhou C, Fan Z, Gu Y, Ge Z, Tao Z, Cui R, Li Y, Zhou G, Huo R, Gao M, Wang D, He W, Zheng M, Zhang S, Xu T.
J Med Chem (2024) 67 : 1147 -1167
PubMed 38197882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.53 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5081048 1 8.82
CHEMBL5569441 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5081048 IC50 = 1.5 nM 8.82
CHEMBL5569441 IC50 = 5.8 nM 8.24