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Compound Detail

CHEMBL3764768

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COc1cc2ncnc(-n3nc(-c4ccccn4)nc3N)c2cc1OCCCNC(=O)OC(C)C

Basic Information

ChEMBL ID CHEMBL3764768
Phase Preclinical
Structure Type MOL
InChI Key IJHWUYUPCVHLDZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
8
Publications
0
Known Names

Molecular Properties

478.5
MW (Da)
2.77
ALogP
11
HBA
2
HBD
152.2
PSA (Ų)
0.34
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N8O4
MW 478.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.22

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine-protein kinase ATM
CHEMBL3797
IC50 6.0 6.0 1000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.9 mL.min-1.kg-1 Canis lupus familiaris
CL 18.8 mL.min-1.kg-1 Homo sapiens
CL 45.1 mL.min-1.kg-1 Rattus norvegicus
CL 329.4 mL.min-1.kg-1 Mus musculus
T1/2 4.0 hr Canis lupus familiaris
T1/2 1.1 hr Homo sapiens
T1/2 1.0 hr Rattus norvegicus
T1/2 0.2 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine