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Assay Detail

CHEMBL4410612

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

ADMET
Inhibition of human dihydrofolate reductase using dihydrofolate as substrate in presence of NADPH by UV-vis spectrophotometry analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Hydrophobic aromatic substituent pyrimethamine analogues as potential antimalarials for pyrimethamine-resistant Plasmodium falciparum.
Saepua S, Sadorn K, Vanichtanankul J, Anukunwithaya T, Rattanajak R, Vitsupakorn D, Kamchonwongpaisan S, Yuthavong Y, Thongpanchang C.
Bioorg Med Chem (2019) 27 : 115158 -115158
PubMed 31685330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.58 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278847 1 8.80
CHEMBL4565928 1 8.06
CHEMBL22148 1 7.98
CHEMBL4553483 1 7.90
CHEMBL4558959 1 7.89
CHEMBL4447272 1 7.87
CHEMBL4590684 1 7.87
CHEMBL4459902 1 7.84
CHEMBL4452609 1 7.74
CHEMBL4437388 1 7.74
CHEMBL4461699 1 7.71
CHEMBL4462327 1 7.66
CHEMBL4515405 1 7.66
CHEMBL4444614 1 7.63
CHEMBL4557136 1 7.56
CHEMBL36 PYRIMETHAMINE 4.0 1 7.55
CHEMBL4586252 1 7.54
CHEMBL4542001 1 7.49
CHEMBL4467953 1 7.48
CHEMBL4546946 1 7.46
CHEMBL4588852 1 7.34
CHEMBL4526752 1 7.31
CHEMBL4566524 1 7.28
CHEMBL4468791 1 7.13
CHEMBL4459356 1 6.29
CHEMBL4441455 1 6.25
CHEMBL4456065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278847 Ki = 1.6 nM 8.80
CHEMBL4565928 Ki = 8.72 nM 8.06
CHEMBL22148 Ki = 10.4 nM 7.98
CHEMBL4553483 Ki = 12.5 nM 7.90
CHEMBL4558959 Ki = 12.77 nM 7.89
CHEMBL4447272 Ki = 13.41 nM 7.87
CHEMBL4590684 Ki = 13.59 nM 7.87
CHEMBL4459902 Ki = 14.36 nM 7.84
CHEMBL4452609 Ki = 18.24 nM 7.74
CHEMBL4437388 Ki = 18.41 nM 7.74
CHEMBL4461699 Ki = 19.55 nM 7.71
CHEMBL4462327 Ki = 21.72 nM 7.66
CHEMBL4515405 Ki = 22.07 nM 7.66
CHEMBL4444614 Ki = 23.42 nM 7.63
CHEMBL4557136 Ki = 27.27 nM 7.56
CHEMBL36 PYRIMETHAMINE Ki = 28.3 nM 7.55
CHEMBL4586252 Ki = 29.05 nM 7.54
CHEMBL4542001 Ki = 32.43 nM 7.49
CHEMBL4467953 Ki = 32.89 nM 7.48
CHEMBL4546946 Ki = 34.84 nM 7.46
CHEMBL4588852 Ki = 45.97 nM 7.34
CHEMBL4526752 Ki = 48.67 nM 7.31
CHEMBL4566524 Ki = 52.39 nM 7.28
CHEMBL4468791 Ki = 74.16 nM 7.13
CHEMBL4459356 Ki = 508.88 nM 6.29
CHEMBL4441455 Ki = 555.55 nM 6.25
CHEMBL4456065 Ki - -