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Compound Detail

CHEMBL44684

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COc1cc(Cc2cnc(N)nc2N)cc(OCCC(=O)NC(CCC(=O)O)C(=O)O)c1Br

Basic Information

ChEMBL ID CHEMBL44684
Phase Preclinical
Structure Type MOL
InChI Key LXVAIRRPWXYFBA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

526.3
MW (Da)
1.21
ALogP
9
HBA
5
HBD
200.0
PSA (Ų)
0.27
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24BrN5O7
MW 526.34
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.08

Activity Summary

Ki 1 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2902
Ki 8.77 8.77 1.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6438320 10.1021/jm00378a025 Dihydrofolate reductase 2

Data from ChEMBL 36 via Core Engine