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Assay Detail

CHEMBL5242447

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

Binding
Binding affinity to full-length C-terminal GFP-tagged human MCT4 incubated for 1 hrs by fluorescence cross-correlation spectroscopy analysis
ChEMBL ↗
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology.
Heinrich T, Sala-Hojman A, Ferretti R, Petersson C, Minguzzi S, Gondela A, Ramaswamy S, Bartosik A, Czauderna F, Crowley L, Wahra P, Schilke H, Böpple P, Dudek Ł, Leś M, Niedziejko P, Olech K, Pawlik H, Włoszczak Ł, Zuchowicz K, Suarez Alvarez JR, Martyka J, Sitek E, Mikulski M, Szczęśniak J, Jäckel S, Krier M, Król M, Wegener A, Gałęzowski M, Nowak M, Becker F, Herhaus C.
J Med Chem (2021) 64 : 11904 -11933
PubMed 34382802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.77 7.21
Ki 13 7.51 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5276884 — — 2 7.96
CHEMBL4802043 MSC-4381 — 2 7.96
CHEMBL5279064 — — 2 7.80
CHEMBL5267752 — — 2 7.77
CHEMBL5267349 — — 2 7.77
CHEMBL5281492 — — 2 7.77
CHEMBL5287351 — — 2 7.54
CHEMBL5287780 — — 2 7.50
CHEMBL5268966 — — 2 7.43
CHEMBL5288904 — — 2 7.29
CHEMBL5265956 — — 2 7.25
CHEMBL5266104 — — 2 7.00
CHEMBL5271816 — — 2 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5276884 — Ki = 11.0 nM 7.96
CHEMBL4802043 MSC-4381 Ki = 11.0 nM 7.96
CHEMBL5279064 — Ki = 16.0 nM 7.80
CHEMBL5267752 — Ki = 17.0 nM 7.77
CHEMBL5281492 — Ki = 17.0 nM 7.77
CHEMBL5267349 — Ki = 17.0 nM 7.77
CHEMBL5287351 — Ki = 29.0 nM 7.54
CHEMBL5287780 — Ki = 32.0 nM 7.50
CHEMBL5268966 — Ki = 37.0 nM 7.43
CHEMBL5288904 — Ki = 51.0 nM 7.29
CHEMBL5265956 — Ki = 56.0 nM 7.25
CHEMBL5281492 — IC50 = 62.0 nM 7.21
CHEMBL4802043 MSC-4381 IC50 = 77.0 nM 7.11
CHEMBL5267752 — IC50 = 79.0 nM 7.10
CHEMBL5267349 — IC50 = 80.0 nM 7.10
CHEMBL5279064 — IC50 = 92.0 nM 7.04
CHEMBL5276884 — IC50 = 99.0 nM 7.00
CHEMBL5266104 — Ki = 99.0 nM 7.00
CHEMBL5287351 — IC50 = 139.0 nM 6.86
CHEMBL5287780 — IC50 = 154.0 nM 6.81
CHEMBL5268966 — IC50 = 215.0 nM 6.67
CHEMBL5271816 — Ki = 222.0 nM 6.65
CHEMBL5288904 — IC50 = 243.0 nM 6.61
CHEMBL5265956 — IC50 = 490.0 nM 6.31
CHEMBL5266104 — IC50 = 579.0 nM 6.24
CHEMBL5271816 — IC50 = 1020.0 nM 5.99