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Compound Detail

CHEMBL302068

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CCC(Cc1ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc1)c1cnc2nc(N)nc(N)c2n1

Basic Information

ChEMBL ID CHEMBL302068
Phase Preclinical
Structure Type MOL
InChI Key BRBJBKGSGUBGLP-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
1.37
ALogP
9
HBA
5
HBD
207.3
PSA (Ų)
0.29
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N7O5
MW 467.49
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.01

Activity Summary

IC50 2 meas. best 8.33
Ki 2 meas. best 5.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 8.33 8.33 4.7 1
Dihydrofolate reductase
CHEMBL202
IC50 7.16 7.16 70.0 1
Dihydrofolate reductase
CHEMBL4564
Ki 5.09 5.09 8200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2296020 10.1021/jm00163a035 Dihydrofolate reductase 3
2296020 10.1021/jm00163a035 L1210 1
2296020 10.1021/jm00163a035 Thymidylate synthase 1
2296020 10.1021/jm00163a035 Unchecked 1
2296020 10.1021/jm00163a035 Bifunctional purine biosynthesis protein ATIC 1

Data from ChEMBL 36 via Core Engine