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Assay Detail

CHEMBL669279

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

Binding
In vitro inhibition of human dihydrofolate reductase
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibitors of Candida albicans dihydrofolate reductase: activity and selectivity of 5-(arylthio)-2,4-diaminoquinazolines.
Chan JH, Hong JS, Kuyper LF, Baccanari DP, Joyner SS, Tansik RL, Boytos CM, Rudolph SK.
J Med Chem (1995) 38 : 3608 -3616
PubMed 7658448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.89 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7492 PIRITREXIM 2.0 1 8.70
CHEMBL121669 1 7.52
CHEMBL334307 1 7.04
CHEMBL123353 1 6.75
CHEMBL121057 1 6.70
CHEMBL338742 1 6.57
CHEMBL333769 1 6.50
CHEMBL121303 1 6.40
CHEMBL121595 1 6.26
CHEMBL100239 1 6.21
CHEMBL420721 1 6.09
CHEMBL83547 1 6.03
CHEMBL118490 1 5.89
CHEMBL121644 1 5.70
CHEMBL329985 1 5.70
CHEMBL310759 1 5.68
CHEMBL124304 1 5.62
CHEMBL413110 1 5.58
CHEMBL36 PYRIMETHAMINE 4.0 1 5.58
CHEMBL118316 1 5.51
CHEMBL330868 1 5.46
CHEMBL123061 1 5.41
CHEMBL122647 1 5.39
CHEMBL333976 1 5.37
CHEMBL120588 1 5.37
CHEMBL120924 1 5.36
CHEMBL122628 1 5.04
CHEMBL121680 1 4.62
CHEMBL120783 1 4.48
CHEMBL328827 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7492 PIRITREXIM IC50 = 2.0 nM 8.70
CHEMBL121669 IC50 = 30.0 nM 7.52
CHEMBL334307 IC50 = 92.0 nM 7.04
CHEMBL123353 IC50 = 180.0 nM 6.75
CHEMBL121057 IC50 = 200.0 nM 6.70
CHEMBL338742 IC50 = 270.0 nM 6.57
CHEMBL333769 IC50 = 320.0 nM 6.50
CHEMBL121303 IC50 = 400.0 nM 6.40
CHEMBL121595 IC50 = 550.0 nM 6.26
CHEMBL100239 IC50 = 620.0 nM 6.21
CHEMBL420721 IC50 = 820.0 nM 6.09
CHEMBL83547 IC50 = 940.0 nM 6.03
CHEMBL118490 IC50 = 1300.0 nM 5.89
CHEMBL121644 IC50 = 2000.0 nM 5.70
CHEMBL329985 IC50 = 2000.0 nM 5.70
CHEMBL310759 IC50 = 2100.0 nM 5.68
CHEMBL124304 IC50 = 2400.0 nM 5.62
CHEMBL413110 IC50 = 2600.0 nM 5.58
CHEMBL36 PYRIMETHAMINE IC50 = 2600.0 nM 5.58
CHEMBL118316 IC50 = 3100.0 nM 5.51
CHEMBL330868 IC50 = 3500.0 nM 5.46
CHEMBL123061 IC50 = 3900.0 nM 5.41
CHEMBL122647 IC50 = 4100.0 nM 5.39
CHEMBL333976 IC50 = 4300.0 nM 5.37
CHEMBL120588 IC50 = 4300.0 nM 5.37
CHEMBL120924 IC50 = 4400.0 nM 5.36
CHEMBL122628 IC50 = 9100.0 nM 5.04
CHEMBL121680 IC50 = 24000.0 nM 4.62
CHEMBL120783 IC50 = 33000.0 nM 4.48
CHEMBL328827 IC50 = 70000.0 nM 4.16
CHEMBL22 TRIMETHOPRIM IC50 = 490000.0 nM -
CHEMBL119 TRIMETREXATE IC50 < 1.0 nM -
CHEMBL334017 IC50 > 10000.0 nM -