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Assay Detail

CHEMBL5521389

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

Binding
Inhibition of MAT2a (unknown origin) using methionine and ATP as substrate assessed as reduction in S-adenosyl-L-methionine formation incubated for 300 mins by RapidFire-Mass Spectrometry analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

S-adenosylmethionine synthase isoform type-2 (CHEMBL3313835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
Atkinson SJ, Bagal SK, Argyrou A, Askin S, Cheung T, Chiarparin E, Coen M, Collie IT, Dale IL, De Fusco C, Dillman K, Evans L, Feron LJ, Foster AJ, Grondine M, Kantae V, Lamont GM, Lamont S, Lynch JT, Nilsson Lill S, Robb GR, Saeh J, Schimpl M, Scott JS, Smith J, Srinivasan B, Tentarelli S, Vazquez-Chantada M, Wagner D, Walsh JJ, Watson D, Williamson B.
J Med Chem (2024) 67 : 4541 -4559
PubMed 38466661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.61 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4573938 1 9.40
CHEMBL5561157 1 9.30
CHEMBL5560496 1 9.10
CHEMBL5562574 1 8.00
CHEMBL5558360 1 7.90
CHEMBL5560583 1 7.20
CHEMBL5563282 1 6.80
CHEMBL5560046 1 6.60
CHEMBL5556711 1 6.10
CHEMBL5557833 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4573938 IC50 = 0.3981 nM 9.40
CHEMBL5561157 IC50 = 0.5012 nM 9.30
CHEMBL5560496 IC50 = 0.7943 nM 9.10
CHEMBL5562574 IC50 = 10.0 nM 8.00
CHEMBL5558360 IC50 = 12.59 nM 7.90
CHEMBL5560583 IC50 = 63.1 nM 7.20
CHEMBL5563282 IC50 = 158.49 nM 6.80
CHEMBL5560046 IC50 = 251.19 nM 6.60
CHEMBL5556711 IC50 = 794.33 nM 6.10
CHEMBL5557833 IC50 = 1995.26 nM 5.70