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Compound Detail

CHEMBL57222

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CCc1nc(N)nc(N)c1-c1ccc(Cl)c([N+]#N)c1.F[B-](F)(F)F

Basic Information

ChEMBL ID CHEMBL57222
Phase Preclinical
Structure Type MOL
InChI Key XGTKBAOJQKDSQR-UHFFFAOYSA-N
Parent Compound CHEMBL142345
Active Moiety CHEMBL142345
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

275.7
MW (Da)
3.01
ALogP
5
HBA
2
HBD
106.0
PSA (Ų)
0.82
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H12BClF4N6
MW 362.53
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 7.64 7.64 23.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 7.5 7.5 32.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9191966 10.1021/jm970050n Dihydrofolate reductase 2
9191966 10.1021/jm970050n Bifunctional dihydrofolate reductase-thymidylate synthase 1
9191966 10.1021/jm970050n Dihydrofolate reductase; P. carinii vs rat 1
9191966 10.1021/jm970050n Unchecked 1

Data from ChEMBL 36 via Core Engine