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Compound Detail

CHEMBL129301

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CC(C)CC(=O)N(C[C@H](CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(=O)O)C(C)C)[C@@H](CC(C)C)C(N)=O

Basic Information

ChEMBL ID CHEMBL129301
Phase Preclinical
Structure Type MOL
InChI Key PAGKTZVACGXGNS-LMOUFGHUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

819.0
MW (Da)
-0.44
ALogP
10
HBA
9
HBD
292.4
PSA (Ų)
0.06
QED
2
Ro5 Violations
26
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H66N8O10
MW 819.01
Aromatic Rings 1
Heavy Atoms 58
NP-Likeness -0.15

Activity Summary

IC50 1 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2304405
IC50 6.79 6.79 162.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor IC50 = 162.0 nM 6.79 Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykini... 1331450

Literature References

PubMed DOI Target Context # Activities
1331450 10.1021/jm00099a024 Substance-K receptor 1

Data from ChEMBL 36 via Core Engine