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Assay Detail

CHEMBL5318008

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

Binding
Inhibition of PHGDH (unknown origin) preincubated for 30 mins followed by substrate addition and measured after 5 mins
32
Total Activities
32
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

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

Publication

Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy.
Gao D, Tang S, Cen Y, Yuan L, Lan X, Li QH, Lin GQ, Huang M, Tian P.
J Med Chem (2023) 66 : 285 -305
PubMed 36594670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.26 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4533417 1 6.97
CHEMBL4545772 1 6.79
CHEMBL5415992 1 5.66
CHEMBL5418330 1 5.62
CHEMBL5435562 1 5.58
CHEMBL5436320 1 5.55
CHEMBL5440487 1 5.50
CHEMBL5418314 1 5.45
CHEMBL5404538 1 5.42
CHEMBL5394206 1 5.32
CHEMBL5412915 1 5.30
CHEMBL5401773 1 5.27
CHEMBL4070806 1 5.21
CHEMBL5413529 1 5.21
CHEMBL5409883 1 5.19
CHEMBL5426021 1 5.17
CHEMBL5413530 1 5.17
CHEMBL5405367 1 5.15
CHEMBL5422286 1 5.13
CHEMBL5411304 1 5.11
CHEMBL5404397 1 5.10
CHEMBL5439942 1 4.96
CHEMBL5403306 1 4.94
CHEMBL5406447 1 4.91
CHEMBL5424581 1 4.90
CHEMBL5419037 1 4.89
CHEMBL5404649 1 4.89
CHEMBL5399957 1 4.80
CHEMBL5427764 1 4.80
CHEMBL5408434 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4533417 IC50 = 106.0 nM 6.97
CHEMBL4545772 IC50 = 162.0 nM 6.79
CHEMBL5415992 IC50 = 2200.0 nM 5.66
CHEMBL5418330 IC50 = 2400.0 nM 5.62
CHEMBL5435562 IC50 = 2600.0 nM 5.58
CHEMBL5436320 IC50 = 2800.0 nM 5.55
CHEMBL5440487 IC50 = 3190.0 nM 5.50
CHEMBL5418314 IC50 = 3590.0 nM 5.45
CHEMBL5404538 IC50 = 3800.0 nM 5.42
CHEMBL5394206 IC50 = 4800.0 nM 5.32
CHEMBL5412915 IC50 = 4960.0 nM 5.30
CHEMBL5401773 IC50 = 5330.0 nM 5.27
CHEMBL4070806 IC50 = 6100.0 nM 5.21
CHEMBL5413529 IC50 = 6160.0 nM 5.21
CHEMBL5409883 IC50 = 6500.0 nM 5.19
CHEMBL5413530 IC50 = 6810.0 nM 5.17
CHEMBL5426021 IC50 = 6700.0 nM 5.17
CHEMBL5405367 IC50 = 7040.0 nM 5.15
CHEMBL5422286 IC50 = 7490.0 nM 5.13
CHEMBL5411304 IC50 = 7740.0 nM 5.11
CHEMBL5404397 IC50 = 7890.0 nM 5.10
CHEMBL5439942 IC50 = 10850.0 nM 4.96
CHEMBL5403306 IC50 = 11380.0 nM 4.94
CHEMBL5406447 IC50 = 12210.0 nM 4.91
CHEMBL5424581 IC50 = 12600.0 nM 4.90
CHEMBL5419037 IC50 = 12960.0 nM 4.89
CHEMBL5404649 IC50 = 12900.0 nM 4.89
CHEMBL5399957 IC50 = 15690.0 nM 4.80
CHEMBL5427764 IC50 = 15800.0 nM 4.80
CHEMBL5408434 IC50 = 17200.0 nM 4.76
CHEMBL5427304 IC50 = 17840.0 nM 4.75
CHEMBL5439263 IC50 = 18500.0 nM 4.73