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Compound Detail

CHEMBL283993

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CCc1nc2c(-c3ccc(OC(F)F)cc3Cl)ccnc2n1C(C)C1CCC1

Basic Information

ChEMBL ID CHEMBL283993
Phase Preclinical
Structure Type MOL
InChI Key NOCSZFMUSSDTEB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

405.9
MW (Da)
6.28
ALogP
4
HBA
0
HBD
39.9
PSA (Ų)
0.48
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22ClF2N3O
MW 405.88
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.41

Activity Summary

Ki 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin releasing factor receptor
CHEMBL2111360
Ki 9.15 9.15 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 795.0 nM Canis lupus familiaris
Cmax 185.0 nM Canis lupus familiaris
T1/2 10.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12467631 10.1016/s0960-894x(02)00833-8 Canis familiaris 3
12467631 10.1016/s0960-894x(02)00833-8 Corticotropin releasing factor receptor 1
12467631 10.1016/s0960-894x(02)00833-8 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine