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Assay Detail

CHEMBL5047545

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Binding
Inhibition of pyruvate carboxylase in human HCCLM3 cell lysate measured upto 24 hrs by PC assay kit
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HCCLM3
Subcellular Lysate
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming.
Sheng Y, Chen Y, Zeng Z, Wu W, Wang J, Ma Y, Lin Y, Zhang J, Huang Y, Li W, Zhu Q, Wei X, Li S, Wisanwattana W, Li F, Liu W, Suksamrarn A, Zhang G, Jiao W, Wang F.
J Med Chem (2022) 65 : 460 -484
PubMed 34931827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.06 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10557 1 8.29
CHEMBL5085855 1 7.19
CHEMBL1794791 OXALOACETATE 2.0 1 7.05
CHEMBL219553 GIGANTOL 1 6.90
CHEMBL374047 MOSCATILIN 1 6.72
CHEMBL254186 1 6.69
CHEMBL5093670 1 6.58
CHEMBL3337992 1 -
CHEMBL426871 1 -
CHEMBL109266 RHAPONTIN 1 -
CHEMBL5089298 1 -
CHEMBL5093275 1 -
CHEMBL5084109 1 -
CHEMBL5076060 1 -
CHEMBL5078918 1 -
CHEMBL475652 HIRCINOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10557 IC50 = 5.184 nM 8.29
CHEMBL5085855 IC50 = 65.0 nM 7.19
CHEMBL1794791 OXALOACETATE IC50 = 88.8 nM 7.05
CHEMBL219553 GIGANTOL IC50 = 125.0 nM 6.90
CHEMBL374047 MOSCATILIN IC50 = 191.0 nM 6.72
CHEMBL254186 IC50 = 204.0 nM 6.69
CHEMBL5093670 IC50 = 264.0 nM 6.58
CHEMBL3337992 IC50 > 50000.0 nM -
CHEMBL426871 IC50 > 50000.0 nM -
CHEMBL109266 RHAPONTIN IC50 > 50000.0 nM -
CHEMBL5089298 IC50 > 50000.0 nM -
CHEMBL5093275 IC50 > 50000.0 nM -
CHEMBL5084109 IC50 > 50000.0 nM -
CHEMBL5076060 IC50 > 50000.0 nM -
CHEMBL5078918 IC50 > 50000.0 nM -
CHEMBL475652 HIRCINOL IC50 > 50000.0 nM -