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Compound Detail

CHEMBL242625

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CN1CCN(C(=O)CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(NC(=O)c3cc4ccccc4s3)CCCC2)CC1

Basic Information

ChEMBL ID CHEMBL242625
Phase Preclinical
Structure Type MOL
InChI Key DRZJIWHMRQXGEA-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

589.8
MW (Da)
2.95
ALogP
6
HBA
3
HBD
110.8
PSA (Ų)
0.34
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39N5O4S
MW 589.76
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.20

Activity Summary

Ki 1 meas. best 8.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2327
Ki 8.97 8.97 1.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor Ki = 1.072 nM 8.97 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 2
17850056 10.1021/jm070289w Caco-2 1

Data from ChEMBL 36 via Core Engine