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Assay Detail

CHEMBL857524

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Binding
Tested for inhibitory activity against thymidylate synthase of L1210 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L1210
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thymidylate synthase (CHEMBL3160)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).
Bavetsias V, Marriott JH, Theti DS, Melin JC, Wilson SC, Jackman AL.
Bioorg Med Chem Lett (2001) 11 : 3015 -3017
PubMed 11714600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.74 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320217 1 9.77
CHEMBL102143 1 9.70
CHEMBL323098 1 9.48
CHEMBL320450 1 9.38
CHEMBL103105 1 9.15
CHEMBL55437 1 9.11
CHEMBL320651 1 8.68
CHEMBL317717 1 8.46
CHEMBL422395 1 7.70
CHEMBL102954 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320217 Ki = 0.17 nM 9.77
CHEMBL102143 Ki = 0.2 nM 9.70
CHEMBL323098 Ki = 0.33 nM 9.48
CHEMBL320450 Ki = 0.42 nM 9.38
CHEMBL103105 Ki = 0.71 nM 9.15
CHEMBL55437 Ki = 0.78 nM 9.11
CHEMBL320651 Ki = 2.1 nM 8.68
CHEMBL317717 Ki = 3.5 nM 8.46
CHEMBL422395 Ki = 20.0 nM 7.70
CHEMBL102954 Ki = 1200.0 nM 5.92