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Assay Detail

CHEMBL823516

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Binding
Inhibition of human Thymidylate synthase
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thymidylate synthase (CHEMBL1952)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones.
Webber SE, Bleckman TM, Attard J, Deal JG, Kathardekar V, Welsh KM, Webber S, Janson CA, Matthews DA, Smith WW.
J Med Chem (1993) 36 : 733 -746
PubMed 8459400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.91 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349723 1 7.96
CHEMBL320775 NOLATREXED 3.0 1 7.80
CHEMBL162145 1 7.75
CHEMBL351885 1 7.62
CHEMBL163411 1 7.34
CHEMBL351606 1 7.30
CHEMBL351403 1 7.24
CHEMBL349969 1 7.24
CHEMBL165453 1 7.19
CHEMBL350130 1 7.18
CHEMBL162613 1 7.11
CHEMBL164624 1 6.92
CHEMBL423282 1 6.92
CHEMBL163410 1 6.89
CHEMBL351840 1 6.23
CHEMBL164289 1 6.19
CHEMBL162498 1 5.96
CHEMBL163096 1 5.68
CHEMBL164569 1 4.72
CHEMBL351839 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349723 Ki = 11.0 nM 7.96
CHEMBL320775 NOLATREXED Ki = 16.0 nM 7.80
CHEMBL162145 Ki = 18.0 nM 7.75
CHEMBL351885 Ki = 24.0 nM 7.62
CHEMBL163411 Ki = 46.0 nM 7.34
CHEMBL351606 Ki = 50.0 nM 7.30
CHEMBL351403 Ki = 58.0 nM 7.24
CHEMBL349969 Ki = 58.0 nM 7.24
CHEMBL165453 Ki = 65.0 nM 7.19
CHEMBL350130 Ki = 66.0 nM 7.18
CHEMBL162613 Ki = 78.0 nM 7.11
CHEMBL164624 Ki = 120.0 nM 6.92
CHEMBL423282 Ki = 120.0 nM 6.92
CHEMBL163410 Ki = 130.0 nM 6.89
CHEMBL351840 Ki = 590.0 nM 6.23
CHEMBL164289 Ki = 640.0 nM 6.19
CHEMBL162498 Ki = 1100.0 nM 5.96
CHEMBL163096 Ki = 2100.0 nM 5.68
CHEMBL164569 Ki = 19000.0 nM 4.72
CHEMBL351839 Ki = 190000.0 nM -