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Compound Detail

CHEMBL387875

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CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1OC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O

Basic Information

ChEMBL ID CHEMBL387875
Phase Preclinical
Structure Type MOL
InChI Key KPZGCJZIVBIZCL-ZQWQDMLBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

917.0
MW (Da)
2.04
ALogP
10
HBA
11
HBD
312.8
PSA (Ų)
0.01
QED
2
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H56N10O9
MW 917.04
Aromatic Rings 5
Heavy Atoms 67
NP-Likeness -0.18

Activity Summary

EC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KiSS-1 receptor
CHEMBL5413
EC50 8.52 8.52 3.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KiSS-1 receptor EC50 = 3.0 nM 8.52 Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calci... 17579384

Literature References

PubMed DOI Target Context # Activities
17579384 10.1021/jm070064l KiSS-1 receptor 3

Data from ChEMBL 36 via Core Engine