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Compound Detail

CHEMBL283740

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CC1(C)N=C(N)N=C(N)N1c1cccc(COc2cccc(C#N)c2)c1

Basic Information

ChEMBL ID CHEMBL283740
Phase Preclinical
Structure Type MOL
InChI Key UHSFYDTWKATRPP-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
2.32
ALogP
7
HBA
2
HBD
113.0
PSA (Ų)
0.88
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 C19H20N6O
MW 348.41
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.99

Activity Summary

Ki 4 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1926
Ki 8.08 8.08 8.3 1
Dihydrofolate reductase
CHEMBL2575
Ki 7.59 7.59 25.7 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL4614
Ki 6.75 6.75 177.8 1
Dihydrofolate reductase
CHEMBL2902
Ki 6.44 6.44 363.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6796688 10.1021/jm00144a010 Lacticaseibacillus casei 2
3934385 10.1021/jm00150a026 Escherichia coli 2
6699880 10.1021/jm00369a019 Dihydrofolate reductase 2
6420569 10.1021/jm00368a006 Dihydrofolate reductase 2
7699713 10.1021/jm00006a016 Dihydrofolate reductase 1
3599028 10.1021/jm00390a017 Bifunctional dihydrofolate reductase-thymidylate synthase 1
6796688 10.1021/jm00144a010 Dihydrofolate reductase 1
7057420 10.1021/jm00344a012 L5178Y 1
7057421 10.1021/jm00344a013 L5178Y 1
3934385 10.1021/jm00150a026 Dihydrofolate reductase type 1 1

Data from ChEMBL 36 via Core Engine