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Assay Detail

CHEMBL2076210

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

Functional
TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
27
Total Activities
23
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Xenopus laevis
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Monocarboxylate transporter 2 (CHEMBL2073718)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes.
Bröer S, Bröer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW.
Biochem J (1999) 341 : 529 -535
PubMed 10417314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 17 - -
Ki 5 4.05 4.10
IC50 4 4.96 5.30
Km 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50 QUERCETIN 3.0 2 5.30
CHEMBL388590 BENZBROMARONE 4.0 2 5.05
CHEMBL45068 PHLORETIN 2 4.85
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID 2 4.62
CHEMBL1162144 PYRUVATE 2.0 1 4.10
CHEMBL445647 2-Oxoisohexanoate 1 4.00
CHEMBL173439 1 -
CHEMBL445874 ADAMANTANEACETIC ACID 1 -
CHEMBL1609 MANDELIC ACID -1.0 1 -
CHEMBL1909428 p-Chloromercuribenzenesulfonate 1 -
CHEMBL2074646 1 -
CHEMBL458328 1 -
CHEMBL63323 NIFLUMIC ACID 2.0 1 -
CHEMBL1256759 5-NITRO-2-PHENYLPROPYLAMINOBENZOIC ACID [NPPB] 1 -
CHEMBL121047 DIBENZYL DISULFIDE 1 -
CHEMBL1374360 MERCURIC CHLORIDE -1.0 1 -
CHEMBL107057 1 -
CHEMBL897 PROBENECID 4.0 1 -
CHEMBL146554 2-Oxoisovalerate 1 -
CHEMBL1230762 ACETOACETIC ACID -1.0 1 -
CHEMBL1162496 3-HYDROXYBUTYRIC ACID, (+/-)- 1.0 1 -
CHEMBL1513985 ANTHRACENE-9-CARBOXYLIC ACID 1 -
CHEMBL358850 D-LACTIC ACID 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50 QUERCETIN IC50 = 5000.0 nM 5.30
CHEMBL388590 BENZBROMARONE IC50 = 9000.0 nM 5.05
CHEMBL45068 PHLORETIN IC50 = 14000.0 nM 4.85
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID IC50 = 24000.0 nM 4.62
CHEMBL1162144 PYRUVATE Ki = 80000.0 nM 4.10
CHEMBL445647 2-Oxoisohexanoate Ki = 100000.0 nM 4.00
CHEMBL173439 Activity = 105.0 % -
CHEMBL445874 ADAMANTANEACETIC ACID Activity = 113.0 % -
CHEMBL1609 MANDELIC ACID Activity = 117.0 % -
CHEMBL1909428 p-Chloromercuribenzenesulfonate Activity = 118.0 % -
CHEMBL2074646 Activity = 119.0 % -
CHEMBL388590 BENZBROMARONE Activity = 12.0 % -
CHEMBL458328 Activity = 125.0 % -
CHEMBL63323 NIFLUMIC ACID Activity = 14.0 % -
CHEMBL50 QUERCETIN Activity = 17.0 % -
CHEMBL1256759 5-NITRO-2-PHENYLPROPYLAMINOBENZOIC ACID [NPPB] Activity = 25.0 % -
CHEMBL45068 PHLORETIN Activity = 3.0 % -
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID Activity = 34.0 % -
CHEMBL1513985 ANTHRACENE-9-CARBOXYLIC ACID Activity = 104.0 % -
CHEMBL1374360 MERCURIC CHLORIDE Activity = 54.0 % -
CHEMBL107057 Activity = 74.0 % -
CHEMBL897 PROBENECID Activity = 88.0 % -
CHEMBL146554 2-Oxoisovalerate Ki = 300000.0 nM -
CHEMBL1230762 ACETOACETIC ACID Ki = 800000.0 nM -
CHEMBL1162496 3-HYDROXYBUTYRIC ACID, (+/-)- Ki = 1200000.0 nM -
CHEMBL358850 D-LACTIC ACID Km = 740000.0 nM -
CHEMBL121047 DIBENZYL DISULFIDE Activity = 44.0 % -