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Assay Detail

CHEMBL665442

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Binding
Inhibitory activity against rat liver dihydrofolate reductase
ChEMBL ↗
66
Total Activities
66
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 (CHEMBL2363) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.
Piper JR, Johnson CA, Krauth CA, Carter RL, Hosmer CA, Queener SF, Borotz SE, Pfefferkorn ER.
J Med Chem (1996) 39 : 1271 -1280
PubMed 8632434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 66 6.43 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7492 PIRITREXIM 2.0 1 8.82
CHEMBL119 TRIMETREXATE 4.0 1 8.52
CHEMBL279680 — — 1 8.28
CHEMBL23532 — — 1 8.27
CHEMBL283518 — — 1 8.19
CHEMBL23021 — — 1 8.00
CHEMBL22623 — — 1 7.89
CHEMBL23963 — — 1 7.77
CHEMBL281648 — — 1 7.70
CHEMBL23227 — — 1 7.64
CHEMBL23382 — — 1 7.54
CHEMBL23569 — — 1 7.51
CHEMBL23211 — — 1 7.26
CHEMBL279983 — — 1 7.21
CHEMBL23416 — — 1 7.14
CHEMBL23092 — — 1 7.14
CHEMBL23867 — — 1 6.96
CHEMBL23383 — — 1 6.92
CHEMBL282948 — — 1 6.89
CHEMBL23374 — — 1 6.87
CHEMBL23220 — — 1 6.85
CHEMBL23713 — — 1 6.82
CHEMBL279705 — — 1 6.80
CHEMBL23244 — — 1 6.75
CHEMBL24007 — — 1 6.72
CHEMBL23705 — — 1 6.64
CHEMBL22924 — — 1 6.64
CHEMBL23076 — — 1 6.64
CHEMBL22672 — — 1 6.52
CHEMBL281131 — — 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7492 PIRITREXIM IC50 = 1.5 nM 8.82
CHEMBL119 TRIMETREXATE IC50 = 3.0 nM 8.52
CHEMBL279680 — IC50 = 5.2 nM 8.28
CHEMBL23532 — IC50 = 5.4 nM 8.27
CHEMBL283518 — IC50 = 6.5 nM 8.19
CHEMBL23021 — IC50 = 10.0 nM 8.00
CHEMBL22623 — IC50 = 13.0 nM 7.89
CHEMBL23963 — IC50 = 17.0 nM 7.77
CHEMBL281648 — IC50 = 20.0 nM 7.70
CHEMBL23227 — IC50 = 23.0 nM 7.64
CHEMBL23382 — IC50 = 29.0 nM 7.54
CHEMBL23569 — IC50 = 31.0 nM 7.51
CHEMBL23211 — IC50 = 55.0 nM 7.26
CHEMBL279983 — IC50 = 61.0 nM 7.21
CHEMBL23092 — IC50 = 73.0 nM 7.14
CHEMBL23416 — IC50 = 72.0 nM 7.14
CHEMBL23867 — IC50 = 110.0 nM 6.96
CHEMBL23383 — IC50 = 120.0 nM 6.92
CHEMBL282948 — IC50 = 130.0 nM 6.89
CHEMBL23374 — IC50 = 135.0 nM 6.87
CHEMBL23220 — IC50 = 140.0 nM 6.85
CHEMBL23713 — IC50 = 150.0 nM 6.82
CHEMBL279705 — IC50 = 160.0 nM 6.80
CHEMBL23244 — IC50 = 180.0 nM 6.75
CHEMBL24007 — IC50 = 190.0 nM 6.72
CHEMBL23705 — IC50 = 230.0 nM 6.64
CHEMBL23076 — IC50 = 230.0 nM 6.64
CHEMBL22924 — IC50 = 230.0 nM 6.64
CHEMBL22672 — IC50 = 300.0 nM 6.52
CHEMBL281131 — IC50 = 320.0 nM 6.50
CHEMBL23272 — IC50 = 330.0 nM 6.48
CHEMBL22677 — IC50 = 370.0 nM 6.43
CHEMBL279679 — IC50 = 370.0 nM 6.43
CHEMBL291239 — IC50 = 430.0 nM 6.37
CHEMBL23454 — IC50 = 460.0 nM 6.34
CHEMBL281803 — IC50 = 460.0 nM 6.34
CHEMBL22543 — IC50 = 470.0 nM 6.33
CHEMBL24344 — IC50 = 500.0 nM 6.30
CHEMBL23844 — IC50 = 530.0 nM 6.28
CHEMBL23911 — IC50 = 520.0 nM 6.28
CHEMBL23584 — IC50 = 550.0 nM 6.26
CHEMBL277217 — IC50 = 600.0 nM 6.22
CHEMBL23492 — IC50 = 720.0 nM 6.14
CHEMBL284544 — IC50 = 770.0 nM 6.11
CHEMBL23288 — IC50 = 810.0 nM 6.09
CHEMBL23919 — IC50 = 880.0 nM 6.06
CHEMBL26006 — IC50 = 1260.0 nM 5.90
CHEMBL23459 — IC50 = 1900.0 nM 5.72
CHEMBL23466 — IC50 = 1900.0 nM 5.72
CHEMBL36 PYRIMETHAMINE IC50 = 2300.0 nM 5.64