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Assay Detail

CHEMBL4375177

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

Binding
Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C]-serine incubated for 72 hrs using [13C]glucose as substrate by LC-MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D-3-phosphoglycerate dehydrogenase (CHEMBL2311243)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor <b>BI-4924</b> Disrupts Serine Biosynthesis.
Weinstabl H, Treu M, Rinnenthal J, Zahn SK, Ettmayer P, Bader G, Dahmann G, Kessler D, Rumpel K, Mischerikow N, Savarese F, Gerstberger T, Mayer M, Zoephel A, Schnitzer R, Sommergruber W, Martinelli P, Arnhof H, Peric-Simov B, Hofbauer KS, Garavel G, Scherbantin Y, Mitzner S, Fett TN, Scholz G, Bruchhaus J, Burkard M, Kousek R, Ciftci T, Sharps B, Schrenk A, Harrer C, Haering D, Wolkerstorfer B, Zhang X, Lv X, Du A, Li D, Li Y, Quant J, Pearson M, McConnell DB.
J Med Chem (2019) 62 : 7976 -7997
PubMed 31365252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.68 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4518579 1 5.70
CHEMBL4520837 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4518579 IC50 = 2000.0 nM 5.70
CHEMBL4520837 IC50 = 2200.0 nM 5.66