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Compound Detail

CHEMBL2042995

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Cc1cccnc1CN1CCC2(CC1)C(=O)N(c1ccc(-c3ccccc3)cc1)c1ncccc12

Basic Information

ChEMBL ID CHEMBL2042995
Phase Preclinical
Structure Type MOL
InChI Key CPBRQQKLCJBJCH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

460.6
MW (Da)
5.66
ALogP
4
HBA
0
HBD
49.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28N4O
MW 460.58
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Egl nine homolog 1
CHEMBL5697
IC50 8.8 8.8 1.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 276.35 ng.hr.mL-1 Rattus norvegicus
CL 59.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 40.0 nM Rattus norvegicus
F - % Rattus norvegicus
T1/2 1.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22364528 10.1021/jm201542d Rattus norvegicus 6
22364528 10.1021/jm201542d Egl nine homolog 1 1
22364528 10.1021/jm201542d Mus musculus 1

Data from ChEMBL 36 via Core Engine