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Compound Detail

CHEMBL569182

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COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(Br)cc1

Basic Information

ChEMBL ID CHEMBL569182
Phase Preclinical
Structure Type MOL
InChI Key FJXHQJTYKKPMGO-ZIAGYGMSSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

434.8
MW (Da)
5.71
ALogP
4
HBA
1
HBD
39.1
PSA (Ų)
0.54
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 C20H21BrClN3O
MW 434.77
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.35

Activity Summary

EC50 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Extracellular calcium-sensing receptor
CHEMBL1878
EC50 7.64 7.64 23.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 36.0 ng/L Rattus norvegicus
AUC 0.444 ng.hr.mL-1 Rattus norvegicus
CL 21.67 mL.min-1.kg-1 Rattus norvegicus
F 24.0 % Rattus norvegicus
MRT 11.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19835382 10.1021/jm9012278 Rattus norvegicus 7
19835382 10.1021/jm9012278 Extracellular calcium-sensing receptor 1

Data from ChEMBL 36 via Core Engine