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Compound Detail

CHEMBL87351

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COc1ccccc1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL87351
Phase Preclinical
Structure Type MOL
InChI Key MHJPVIGLQHLUFI-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

341.4
MW (Da)
4.92
ALogP
4
HBA
0
HBD
39.9
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19N3O
MW 341.41
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.13

Activity Summary

IC50 2 meas. best 5.77
Ki 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V1a receptor
CHEMBL1889
Ki 6.92 6.92 120.0 1
Sodium- and chloride-dependent glycine transporter 2
CHEMBL3195
IC50 5.77 5.77 1700.0 1
Sodium- and chloride-dependent glycine transporter 1
CHEMBL4556
IC50 5.75 5.75 1800.0 1
Vasopressin V2 receptor
CHEMBL1790
Ki 5.61 5.61 2460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21141920 10.1021/jm101031u ADMET 2
12036368 10.1021/jm010544r Vasopressin V1a receptor 1
12036368 10.1021/jm010544r Vasopressin V2 receptor 1
12036368 10.1021/jm010544r Unchecked 1
21141920 10.1021/jm101031u Sodium- and chloride-dependent glycine transporter 1 1
21141920 10.1021/jm101031u Sodium- and chloride-dependent glycine transporter 2 1
21141920 10.1021/jm101031u Unchecked 1

Data from ChEMBL 36 via Core Engine