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Assay Detail

CHEMBL5732732

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Binding
Assay 4: MCT1-Mediated Lactate Transport in BT20 Breast Cancer Cells: MCT1 activity may be measured using BT-20 breast cancer cells that express high native levels of MCT1, but do not express MCT4 and are known to those with skill in the art. Preparation of BCECF loaded cells are as described for Assay 1. Lactate transport assay is as described for Assay 1, except 10 mM L-lactate (rather than 50 mM) is added.
ChEMBL ↗
246
Total Activities
81
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Malignant T-cell-amplified sequence 1 (CHEMBL5724622) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

MCT4 inhibitors for treating disease
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 82 4.77 7.26
kon 82 - -
k_off 82 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5981118 — — 3 7.26
CHEMBL5874865 — — 3 7.00
CHEMBL6018589 — — 3 7.00
CHEMBL5898165 — — 3 6.69
CHEMBL5904074 — — 3 6.69
CHEMBL6031816 — — 3 6.52
CHEMBL6052282 — — 3 6.52
CHEMBL5883085 — — 3 6.52
CHEMBL5918774 — — 3 6.40
CHEMBL5764687 — — 3 6.39
CHEMBL6017525 — — 3 6.39
CHEMBL5985401 — — 3 6.34
CHEMBL6032683 — — 3 5.22
CHEMBL5748717 — — 3 5.05
CHEMBL5929597 — — 3 5.00
CHEMBL5770368 — — 3 4.96
CHEMBL5874781 — — 3 4.96
CHEMBL5792832 — — 3 4.96
CHEMBL5979706 — — 3 4.92
CHEMBL5919124 — — 3 4.89
CHEMBL5807436 — — 3 4.82
CHEMBL5787646 — — 3 4.82
CHEMBL5871500 — — 3 4.80
CHEMBL5802693 — — 3 4.80
CHEMBL5868830 — — 3 4.77
CHEMBL5775755 — — 3 4.77
CHEMBL5998971 — — 3 4.77
CHEMBL5830820 — — 3 4.60
CHEMBL5946556 — — 3 4.58
CHEMBL5807366 — — 3 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5981118 — IC50 = 54.5 nM 7.26
CHEMBL6018589 — IC50 = 100.0 nM 7.00
CHEMBL5874865 — IC50 = 100.0 nM 7.00
CHEMBL5898165 — IC50 = 204.0 nM 6.69
CHEMBL5904074 — IC50 = 204.0 nM 6.69
CHEMBL5883085 — IC50 = 303.0 nM 6.52
CHEMBL6052282 — IC50 = 303.0 nM 6.52
CHEMBL6031816 — IC50 = 302.0 nM 6.52
CHEMBL5918774 — IC50 = 400.0 nM 6.40
CHEMBL6017525 — IC50 = 404.0 nM 6.39
CHEMBL5764687 — IC50 = 404.0 nM 6.39
CHEMBL5985401 — IC50 = 454.0 nM 6.34
CHEMBL6032683 — IC50 = 6000.0 nM 5.22
CHEMBL5748717 — IC50 = 9000.0 nM 5.05
CHEMBL5929597 — IC50 = 10000.0 nM 5.00
CHEMBL5874781 — IC50 = 11000.0 nM 4.96
CHEMBL5770368 — IC50 = 11000.0 nM 4.96
CHEMBL5792832 — IC50 = 11000.0 nM 4.96
CHEMBL5979706 — IC50 = 12000.0 nM 4.92
CHEMBL5919124 — IC50 = 13000.0 nM 4.89
CHEMBL5787646 — IC50 = 15000.0 nM 4.82
CHEMBL5807436 — IC50 = 15000.0 nM 4.82
CHEMBL5802693 — IC50 = 16000.0 nM 4.80
CHEMBL5871500 — IC50 = 16000.0 nM 4.80
CHEMBL5775755 — IC50 = 17000.0 nM 4.77
CHEMBL5868830 — IC50 = 17000.0 nM 4.77
CHEMBL5998971 — IC50 = 17000.0 nM 4.77
CHEMBL5830820 — IC50 = 25000.0 nM 4.60
CHEMBL5946556 — IC50 = 26000.0 nM 4.58
CHEMBL6012653 — IC50 = 27000.0 nM 4.57
CHEMBL5978952 — IC50 = 27000.0 nM 4.57
CHEMBL5807366 — IC50 = 27000.0 nM 4.57
CHEMBL6025808 — IC50 = 27000.0 nM 4.57
CHEMBL5920914 — IC50 = 29000.0 nM 4.54
CHEMBL6061357 — IC50 = 29000.0 nM 4.54
CHEMBL5774880 — IC50 = 33000.0 nM 4.48
CHEMBL5772596 — IC50 = 33000.0 nM 4.48
CHEMBL5935723 — IC50 = 33000.0 nM 4.48
CHEMBL5855198 — IC50 = 34000.0 nM 4.47
CHEMBL5854479 — IC50 = 38000.0 nM 4.42
CHEMBL5754446 — IC50 = 39000.0 nM 4.41
CHEMBL5841550 — IC50 = 42000.0 nM 4.38
CHEMBL5935974 — IC50 = 44000.0 nM 4.36
CHEMBL5765868 — IC50 = 45000.0 nM 4.35
CHEMBL5971853 — IC50 = 45000.0 nM 4.35
CHEMBL6014217 — IC50 = 45000.0 nM 4.35
CHEMBL6022210 — IC50 = 45000.0 nM 4.35
CHEMBL5803742 — IC50 = 46000.0 nM 4.34
CHEMBL5942168 — IC50 = 47000.0 nM 4.33
CHEMBL6027638 — IC50 = 50000.0 nM 4.30