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Compound Detail

CHEMBL161151

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Cc1ccnc(N2CCN(CCc3c(C)n4c5c(cc(NC(=O)c6ccccc6)cc35)CCC4)CC2)c1

Basic Information

ChEMBL ID CHEMBL161151
Phase Preclinical
Structure Type MOL
InChI Key RXLNEEMRNQZQSQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

493.7
MW (Da)
5.22
ALogP
5
HBA
1
HBD
53.4
PSA (Ų)
0.40
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 C31H35N5O
MW 493.66
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.59

Activity Summary

IC50 1 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cavia porcellus
CHEMBL369
IC50 7.07 7.07 86.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cavia porcellus IC50 = 86.0 nM 7.07 Ability to inhibit histamine-induced contractions of isolated guinea pig ileum 7861415

Literature References

PubMed DOI Target Context # Activities
7861415 10.1021/jm00004a013 Cavia porcellus 1
7861415 10.1021/jm00004a013 Oryctolagus cuniculus 1
7861415 10.1021/jm00004a013 Rattus norvegicus 1
7861415 10.1021/jm00004a013 Polyunsaturated fatty acid 5-lipoxygenase 1

Data from ChEMBL 36 via Core Engine