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Compound Detail

CHEMBL3115740

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COc1ccc(/C=C2\CCCC3=C(c4ccc(OC)c(OC)c4)Nc4cc(C)c(C)cc4N=C32)cc1OC

Basic Information

ChEMBL ID CHEMBL3115740
Phase Preclinical
Structure Type MOL
InChI Key FIXIJHRDPFWKAZ-CJLVFECKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

510.6
MW (Da)
7.51
ALogP
6
HBA
1
HBD
61.3
PSA (Ų)
0.37
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34N2O4
MW 510.63
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.01

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1075051
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dihydrofolate reductase IC50 = 4.0 nM 8.4 Inhibition of bovine liver DHFR measured for every 1 min of 10 mins 24469112

Literature References

PubMed DOI Target Context # Activities
24469112 10.1016/j.ejmech.2014.01.004 Dihydrofolate reductase 2

Data from ChEMBL 36 via Core Engine