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Assay Detail

CHEMBL4835539

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

Functional
Antiproliferative activity against MATP-null human HCT-116 cells isogenic cell model assessed as maximal cell growth inhibition at 20 uM incubated for 96 hrs by Cell Titer-Glo assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous <i>MTAP</i> Deletion.
Konteatis Z, Travins J, Gross S, Marjon K, Barnett A, Mandley E, Nicolay B, Nagaraja R, Chen Y, Sun Y, Liu Z, Yu J, Ye Z, Jiang F, Wei W, Fang C, Gao Y, Kalev P, Hyer ML, DeLaBarre B, Jin L, Padyana AK, Dang L, Murtie J, Biller SA, Sui Z, Marks KM.
J Med Chem (2021) 64 : 4430 -4449
PubMed 33829783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.89 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4521249 1 7.14
CHEMBL4558617 1 7.10
CHEMBL4573938 1 6.59
CHEMBL4529030 1 6.39
CHEMBL4584451 1 6.37
CHEMBL4514699 1 6.28
CHEMBL4582312 1 6.28
CHEMBL4568226 1 6.10
CHEMBL4585665 1 6.09
CHEMBL4865263 1 4.14
CHEMBL4874436 1 4.12
CHEMBL4878283 1 4.09
CHEMBL4559088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4521249 IC50 = 73.0 nM 7.14
CHEMBL4558617 IC50 = 80.0 nM 7.10
CHEMBL4573938 IC50 = 257.0 nM 6.59
CHEMBL4529030 IC50 = 409.0 nM 6.39
CHEMBL4584451 IC50 = 430.0 nM 6.37
CHEMBL4514699 IC50 = 527.0 nM 6.28
CHEMBL4582312 IC50 = 522.0 nM 6.28
CHEMBL4568226 IC50 = 793.0 nM 6.10
CHEMBL4585665 IC50 = 812.0 nM 6.09
CHEMBL4865263 IC50 = 72000.0 nM 4.14
CHEMBL4874436 IC50 = 75000.0 nM 4.12
CHEMBL4878283 IC50 = 82000.0 nM 4.09
CHEMBL4559088 IC50 = 892000.0 nM -