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Compound Detail

CHEMBL164387

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CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1.O=C(O)CC(O)(CC(=O)O)C(=O)O

Basic Information

ChEMBL ID CHEMBL164387
Phase Preclinical
Structure Type MOL
InChI Key NNNCWYSCDJPERM-UHFFFAOYSA-N
Parent Compound CHEMBL1181319
Active Moiety CHEMBL1181319
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

644.2
MW (Da)
6.66
ALogP
5
HBA
1
HBD
77.9
PSA (Ų)
0.23
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H42ClN5O10
MW 836.30
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -1.23

Activity Summary

IC50 1 meas. best 7.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V2 receptor
CHEMBL1790
IC50 7.94 7.94 11.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10782686 10.1016/s0960-894x(00)00095-0 Rattus norvegicus 1
10782686 10.1016/s0960-894x(00)00095-0 Vasopressin V2 receptor 1
10782686 10.1016/s0960-894x(00)00095-0 ADMET 1

Data from ChEMBL 36 via Core Engine