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Compound Detail

CHEMBL1807275

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O=C(NCCCO)[C@@H](Cc1ccc(Cl)cc1)NC(=O)C1(c2ccc(Cl)cc2)CCC1

Basic Information

ChEMBL ID CHEMBL1807275
Phase Preclinical
Structure Type MOL
InChI Key WTBZESIEEBBAGY-HXUWFJFHSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

449.4
MW (Da)
3.64
ALogP
3
HBA
3
HBD
78.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26Cl2N2O3
MW 449.38
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.48

Activity Summary

Ki 1 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V1a receptor
CHEMBL1889
Ki 7.55 7.55 28.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 180.0 mL.min-1.g-1 Homo sapiens
CL 270.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vasopressin V1a receptor Ki = 28.18 nM 7.55 Displacement of [3H]AVP from human V1A receptor expressed in CHO cells 21700453

Literature References

PubMed DOI Target Context # Activities
21700453 10.1016/j.bmcl.2011.05.092 Vasopressin V1a receptor 2
21700453 10.1016/j.bmcl.2011.05.092 Liver microsomes 2
21700453 10.1016/j.bmcl.2011.05.092 Caco-2 2

Data from ChEMBL 36 via Core Engine