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Compound Detail

CHEMBL1807264

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O=C(Cc1ccc(Cl)cc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)NCCCO

Basic Information

ChEMBL ID CHEMBL1807264
Phase Preclinical
Structure Type MOL
InChI Key FJSRYIOGYAKWJT-GOSISDBHSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

409.3
MW (Da)
2.76
ALogP
3
HBA
3
HBD
78.4
PSA (Ų)
0.56
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 C20H22Cl2N2O3
MW 409.31
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.57

Activity Summary

Ki 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V1a receptor
CHEMBL1889
Ki 8.15 8.15 7.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.g-1 Homo sapiens
CL 101.0 mL.min-1.g-1 Rattus norvegicus
CL 40.0 mL.min-1.kg-1 Rattus norvegicus
F 43.0 % Rattus norvegicus
T1/2 0.74 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vasopressin V1a receptor Ki = 7.079 nM 8.15 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 Rattus norvegicus 4
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