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Compound Detail

CHEMBL243071

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CN(C(=O)c1cc2ccccc2s1)C1(C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCN2CCOCC2)CCCC1

Basic Information

ChEMBL ID CHEMBL243071
Phase Preclinical
Structure Type MOL
InChI Key CQWNINTZIMKGDV-AREMUKBSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

576.8
MW (Da)
3.85
ALogP
6
HBA
2
HBD
91.0
PSA (Ų)
0.34
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H40N4O4S
MW 576.76
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -1.15

Activity Summary

Ki 1 meas. best 7.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2327
Ki 7.61 7.61 24.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor Ki = 24.55 nM 7.61 Displacement of [125I]neurokinin A from human recombinant NK2 receptor 17850056

Literature References

PubMed DOI Target Context # Activities
17850056 10.1021/jm070289w Substance-K receptor 1
17850056 10.1021/jm070289w Caco-2 1

Data from ChEMBL 36 via Core Engine