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Assay Detail

CHEMBL3584796

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Binding
Inhibition of MCT1-mediated lactate transport in rat RBE4 cells incubated for 15 mins by [14C]-lactate uptake assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RBE4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Monocarboxylate transporter 1 (CHEMBL2073709)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Monocarboxylate transporter 1 inhibitors as potential anticancer agents.
Gurrapu S, Jonnalagadda SK, Alam MA, Nelson GL, Sneve MG, Drewes LR, Mereddy VR.
ACS Med Chem Lett (2015) 6 : 558 -561
PubMed 26005533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.03 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3582422 1 8.10
CHEMBL3582419 1 8.05
CHEMBL3582408 1 8.00
CHEMBL3582423 1 7.96
CHEMBL3582420 1 7.96
CHEMBL3582418 1 7.92
CHEMBL3582426 1 7.60
CHEMBL3582424 1 7.54
CHEMBL3582409 1 7.52
CHEMBL3582415 1 7.52
CHEMBL3582421 1 7.47
CHEMBL3582425 1 7.32
CHEMBL3582407 1 7.16
CHEMBL3582416 1 7.16
CHEMBL3582410 1 7.00
CHEMBL3582413 1 6.96
CHEMBL77436 1 6.85
CHEMBL3582411 1 6.85
CHEMBL3582417 1 6.85
CHEMBL3582414 1 6.40
CHEMBL3582406 1 6.30
CHEMBL77524 1 6.30
CHEMBL309866 1 6.30
CHEMBL3582405 1 6.30
CHEMBL3582404 1 6.30
CHEMBL3582403 1 6.30
CHEMBL78184 1 6.30
CHEMBL3582402 1 6.30
CHEMBL77278 1 6.30
CHEMBL3582412 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3582422 IC50 = 8.0 nM 8.10
CHEMBL3582419 IC50 = 9.0 nM 8.05
CHEMBL3582408 IC50 = 10.0 nM 8.00
CHEMBL3582423 IC50 = 11.0 nM 7.96
CHEMBL3582420 IC50 = 11.0 nM 7.96
CHEMBL3582418 IC50 = 12.0 nM 7.92
CHEMBL3582426 IC50 = 25.0 nM 7.60
CHEMBL3582424 IC50 = 29.0 nM 7.54
CHEMBL3582409 IC50 = 30.0 nM 7.52
CHEMBL3582415 IC50 = 30.0 nM 7.52
CHEMBL3582421 IC50 = 34.0 nM 7.47
CHEMBL3582425 IC50 = 48.0 nM 7.32
CHEMBL3582407 IC50 = 70.0 nM 7.16
CHEMBL3582416 IC50 = 70.0 nM 7.16
CHEMBL3582410 IC50 = 100.0 nM 7.00
CHEMBL3582413 IC50 = 110.0 nM 6.96
CHEMBL77436 IC50 = 140.0 nM 6.85
CHEMBL3582411 IC50 = 140.0 nM 6.85
CHEMBL3582417 IC50 = 140.0 nM 6.85
CHEMBL3582414 IC50 = 400.0 nM 6.40
CHEMBL3582406 IC50 = 500.0 nM 6.30
CHEMBL77524 IC50 = 500.0 nM 6.30
CHEMBL309866 IC50 = 500.0 nM 6.30
CHEMBL3582405 IC50 = 500.0 nM 6.30
CHEMBL3582404 IC50 = 500.0 nM 6.30
CHEMBL3582403 IC50 = 500.0 nM 6.30
CHEMBL78184 IC50 = 500.0 nM 6.30
CHEMBL3582402 IC50 = 500.0 nM 6.30
CHEMBL77278 IC50 = 500.0 nM 6.30
CHEMBL3582412 IC50 = 880.0 nM 6.06