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Compound Detail

CHEMBL66077

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Nc1nc(N)c2[nH]c(-c3ccccc3)nc2n1

Basic Information

ChEMBL ID CHEMBL66077
Phase Preclinical
Structure Type MOL
InChI Key WGJICLLGFIVHNE-UHFFFAOYSA-N
3
Targets
10
Activities
3
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

226.2
MW (Da)
1.18
ALogP
5
HBA
3
HBD
106.5
PSA (Ų)
0.58
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H10N6
MW 226.24
Aromatic Rings 3
Heavy Atoms 17
NP-Likeness -0.55

Activity Summary

IC50 8 meas. best 4.55
Kd 1 meas. best 4.09
Ki 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 4.55 4.55 28000.0 3
Dihydrofolate reductase
CHEMBL2363
IC50 4.22 4.22 59900.0 3
Venus kinase receptor 2
CHEMBL5169215
Kd 4.09 4.09 82000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9301665 10.1021/jm970271t Dihydrofolate reductase 2
2165159 10.1021/jm00170a005 Phosphatidylinositol 4-kinase, PI4K 2
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 2
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 2
9301665 10.1021/jm970271t Bifunctional dihydrofolate reductase-thymidylate synthase 1
9301665 10.1021/jm970271t Dihydrofolate reductase; P. carinii vs rat 1
9301665 10.1021/jm970271t Dihydrofolate reductase; T. gondii vs rat 1
- 10.6019/CHEMBL3988181 Unchecked 1
36385939 10.1021/acsmedchemlett.2c00248 Venus kinase receptor 2 1
36385939 10.1021/acsmedchemlett.2c00248 Schistosoma mansoni 1

Data from ChEMBL 36 via Core Engine