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Compound Detail

CHEMBL168449

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COCCN(Cc1ccccc1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br

Basic Information

ChEMBL ID CHEMBL168449
Phase Preclinical
Structure Type MOL
InChI Key XVAQMBKVKIZPPY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
5
Publications
0
Known Names

Molecular Properties

495.4
MW (Da)
5.06
ALogP
7
HBA
0
HBD
69.0
PSA (Ų)
0.34
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27BrN6O
MW 495.43
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.47

Activity Summary

Ki 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin-releasing factor receptor 1
CHEMBL1800
Ki 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 67.87 ng.hr.mL-1 Rattus norvegicus
AUC 181.18 ng.hr.mL-1 Canis lupus familiaris
CL 8.717 mL.min-1.kg-1 Canis lupus familiaris
Cmax 12.5 nM Rattus norvegicus
Cmax 39.04 nM Canis lupus familiaris
F 15.5 % Rattus norvegicus
F 7.3 % Canis lupus familiaris
T1/2 46.7 hr Canis lupus familiaris
Tmax 0.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10072681 10.1021/jm980224g Canis familiaris 6
10072681 10.1021/jm980224g Rattus norvegicus 3
10072681 10.1021/jm980224g ADMET 2
10072681 10.1021/jm980224g Corticotropin-releasing factor receptor 1 1
10072681 10.1021/jm980224g No relevant target 1

Data from ChEMBL 36 via Core Engine