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Assay Detail

CHEMBL2444904

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

Binding
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SiHa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Monocarboxylate transporter 4 (CHEMBL2073663)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells.
Draoui N, Schicke O, Fernandes A, Drozak X, Nahra F, Dumont A, Douxfils J, Hermans E, Dogné JM, Corbau R, Marchand A, Chaltin P, Sonveaux P, Feron O, Riant O.
Bioorg Med Chem (2013) 21 : 7107 -7117
PubMed 24095010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.76 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442509 1 7.23
CHEMBL2442512 1 6.14
CHEMBL1303766 1 6.07
CHEMBL2442515 1 5.90
CHEMBL2442510 1 5.85
CHEMBL2442513 1 5.72
CHEMBL1830821 1 5.64
CHEMBL2442514 1 5.62
CHEMBL2442508 1 5.10
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID 1 4.36
CHEMBL2442511 1 -
CHEMBL2442516 1 -
CHEMBL2442517 1 -
CHEMBL2442503 1 -
CHEMBL2442504 1 -
CHEMBL2442505 1 -
CHEMBL2442506 1 -
CHEMBL2442507 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442509 IC50 = 59.0 nM 7.23
CHEMBL2442512 IC50 = 730.0 nM 6.14
CHEMBL1303766 IC50 = 860.0 nM 6.07
CHEMBL2442515 IC50 = 1250.0 nM 5.90
CHEMBL2442510 IC50 = 1400.0 nM 5.85
CHEMBL2442513 IC50 = 1900.0 nM 5.72
CHEMBL1830821 IC50 = 2300.0 nM 5.64
CHEMBL2442514 IC50 = 2400.0 nM 5.62
CHEMBL2442508 IC50 = 7900.0 nM 5.10
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID IC50 = 43500.0 nM 4.36
CHEMBL2442511 IC50 > 30000.0 nM -
CHEMBL2442516 IC50 > 30000.0 nM -
CHEMBL2442517 IC50 > 30000.0 nM -
CHEMBL2442503 IC50 > 30000.0 nM -
CHEMBL2442504 IC50 > 30000.0 nM -
CHEMBL2442505 IC50 > 30000.0 nM -
CHEMBL2442506 IC50 > 30000.0 nM -
CHEMBL2442507 IC50 > 30000.0 nM -