Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4835544

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

Functional
Inhibition of SAM production in human HCT-116 cells isogenic cell model measured after 72 hrs by LC-MS/MS analysis
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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.00 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4559088 1 8.10
CHEMBL4584451 1 7.82
CHEMBL4529030 1 7.80
CHEMBL4521249 1 7.75
CHEMBL4558617 1 7.68
CHEMBL4568226 1 7.60
CHEMBL4585665 1 7.19
CHEMBL4560666 1 7.00
CHEMBL4865263 1 6.97
CHEMBL4878283 1 6.23
CHEMBL4874436 1 5.12
CHEMBL4573938 1 4.70
CHEMBL4582312 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4559088 IC50 = 8.0 nM 8.10
CHEMBL4584451 IC50 = 15.0 nM 7.82
CHEMBL4529030 IC50 = 16.0 nM 7.80
CHEMBL4521249 IC50 = 18.0 nM 7.75
CHEMBL4558617 IC50 = 21.0 nM 7.68
CHEMBL4568226 IC50 = 25.0 nM 7.60
CHEMBL4585665 IC50 = 65.0 nM 7.19
CHEMBL4560666 IC50 = 100.0 nM 7.00
CHEMBL4865263 IC50 = 106.0 nM 6.97
CHEMBL4878283 IC50 = 588.0 nM 6.23
CHEMBL4874436 IC50 = 7650.0 nM 5.12
CHEMBL4573938 IC50 = 20000.0 nM 4.70
CHEMBL4582312 IC50 - -