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Compound Detail

CHEMBL362453

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CCCCC(c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1

Basic Information

ChEMBL ID CHEMBL362453
Phase Preclinical
Structure Type MOL
InChI Key SYBPBURKXDRONN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
2
Publications
0
Known Names

Molecular Properties

445.0
MW (Da)
6.43
ALogP
5
HBA
0
HBD
43.2
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30ClFN4O
MW 444.98
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.09

Activity Summary

Ki 1 meas. best 8.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin-releasing factor receptor 1
CHEMBL1800
Ki 8.14 8.14 7.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1013.0 ng.hr.mL-1 Rattus norvegicus
CL 27.7 mL.min-1.kg-1 Rattus norvegicus
Cmax 651.71 nM Rattus norvegicus
F 84.0 % Rattus norvegicus
T1/2 3.3 hr Rattus norvegicus
Tmax 0.5 hr Rattus norvegicus
Vd 7.8 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15743196 10.1021/jm049339c ADMET 8
15743196 10.1021/jm049339c Corticotropin-releasing factor receptor 1 1

Data from ChEMBL 36 via Core Engine