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Assay Detail

CHEMBL844164

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Binding
Inhibition of thymidylate synthase from L1210 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type L1210
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thymidylate synthase (CHEMBL3160)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogues.
Thornton TJ, Jackman AL, Marsham PR, O'Connor BM, Bishop JA, Calvert AH.
J Med Chem (1992) 35 : 2321 -2327
PubMed 1613755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.45 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169981 1 7.70
CHEMBL434209 1 7.40
CHEMBL75291 1 7.10
CHEMBL307914 1 6.92
CHEMBL40321 1 6.52
CHEMBL73902 1 6.22
CHEMBL420935 1 6.02
CHEMBL77314 1 6.00
CHEMBL419092 1 5.96
CHEMBL73971 1 5.94
CHEMBL307399 1 5.84
CHEMBL420204 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169981 IC50 = 20.0 nM 7.70
CHEMBL434209 IC50 = 40.0 nM 7.40
CHEMBL75291 IC50 = 80.0 nM 7.10
CHEMBL307914 IC50 = 120.0 nM 6.92
CHEMBL40321 IC50 = 300.0 nM 6.52
CHEMBL73902 IC50 = 600.0 nM 6.22
CHEMBL420935 IC50 = 950.0 nM 6.02
CHEMBL77314 IC50 = 1000.0 nM 6.00
CHEMBL419092 IC50 = 1100.0 nM 5.96
CHEMBL73971 IC50 = 1140.0 nM 5.94
CHEMBL307399 IC50 = 1430.0 nM 5.84
CHEMBL420204 IC50 = 1700.0 nM 5.77