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Compound Detail

CHEMBL3787397

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CC1(C)N=C(N)N=C(N)N1c1cccc(C(=O)/C=C/c2ccccc2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3787397
Phase Preclinical
Structure Type MOL
InChI Key CKRVIIJGISKSDA-CALJPSDSSA-N
Parent Compound CHEMBL3787778
Active Moiety CHEMBL3787778
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

347.4
MW (Da)
2.77
ALogP
6
HBA
2
HBD
97.1
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22ClN5O
MW 383.88
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.28

Activity Summary

IC50 3 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 5.62 5.62 2400.0 1
Unchecked
CHEMBL612545
IC50 5.0 4.9 10100.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26994844 10.1016/j.ejmech.2016.03.002 MCF7 2
26994844 10.1016/j.ejmech.2016.03.002 NON-PROTEIN TARGET 2
26994844 10.1016/j.ejmech.2016.03.002 Unchecked 2
26994844 10.1016/j.ejmech.2016.03.002 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine