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Compound Detail

CHEMBL2146615

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COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(NC(C)=O)c3)CC2)C(=O)N1.Cl

Basic Information

ChEMBL ID CHEMBL2146615
Phase Preclinical
Structure Type MOL
InChI Key PRHMKHZSQPQGCD-JCOPYZAKSA-N
Parent Compound CHEMBL185271
Active Moiety CHEMBL185271
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

613.7
MW (Da)
4.04
ALogP
7
HBA
3
HBD
129.3
PSA (Ų)
0.27
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 C31H38ClF2N5O6
MW 650.12
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -1.29

Activity Summary

Kd 1 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
Kd 9.74 9.74 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanin-concentrating hormone receptor 1 Kd = 0.18 nM 9.74 Binding affinity to human MCHR1 expressed in COS7 cells 22921745

Literature References

PubMed DOI Target Context # Activities
22921745 10.1016/j.bmc.2012.07.051 Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine