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Compound Detail

CHEMBL524616

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COCC(COC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12

Basic Information

ChEMBL ID CHEMBL524616
Phase Preclinical
Structure Type MOL
InChI Key XOPNJTADGPQJEJ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
2.80
ALogP
8
HBA
1
HBD
82.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27N5O3
MW 385.47
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.03

Activity Summary

IC50 1 meas. best 8.01
Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin-releasing factor receptor 1
CHEMBL1800
Ki 8.7 8.7 2.0 1
Corticotropin-releasing factor receptor 1
CHEMBL4649
IC50 8.01 8.01 9.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18672365 10.1016/j.bmcl.2008.07.063 Corticotropin-releasing factor receptor 1 1
19361210 10.1021/jm9000242 Corticotropin-releasing factor receptor 1 1

Data from ChEMBL 36 via Core Engine