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Compound Detail

CHEMBL568606

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CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C

Basic Information

ChEMBL ID CHEMBL568606
Phase Preclinical
Structure Type MOL
InChI Key DXVNLEPWBPMCOF-UHFFFAOYSA-N
1
Targets
3
Activities
2
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

383.5
MW (Da)
3.61
ALogP
7
HBA
0
HBD
65.3
PSA (Ų)
0.59
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 C21H29N5O2
MW 383.50
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.77

Activity Summary

Ki 2 meas. best 7.89
Kd 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin-releasing factor receptor 1
CHEMBL1800
Ki 7.89 7.89 13.0 2
Corticotropin-releasing factor receptor 1
CHEMBL1800
Kd 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 172.0 ug ml-1 Homo sapiens
CL 23.0 ug ml-1 Rattus norvegicus
CL 172.0 ug ml-1 Homo sapiens
CL 23.0 ug ml-1 Rattus norvegicus
T1/2 0.3 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21889333 10.1016/j.bmcl.2011.08.040 Corticotropin-releasing factor receptor 1 4
19782566 10.1016/j.bmcl.2009.09.016 Liver microsomes 2
21889333 10.1016/j.bmcl.2011.08.040 Liver microsomes 2
19782566 10.1016/j.bmcl.2009.09.016 Corticotropin-releasing factor receptor 1 1

Data from ChEMBL 36 via Core Engine