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Compound Detail

CHEMBL367815

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O=C1CCN(C2CN(CC[C@]3(c4ccc(Cl)c(Cl)c4)CCC(=O)N(CC4CCC(F)(F)CC4)C3)C2)CC1

Basic Information

ChEMBL ID CHEMBL367815
Phase Preclinical
Structure Type MOL
InChI Key HFWUHIICTJEDKT-HHHXNRCGSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

556.5
MW (Da)
5.42
ALogP
4
HBA
0
HBD
43.9
PSA (Ų)
0.45
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H37Cl2F2N3O2
MW 556.53
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness -0.39

Activity Summary

IC50 1 meas. best 8.5
Kd 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL3433
Kd 9.7 9.7 0.2 1
Substance-K receptor
CHEMBL2327
IC50 8.5 8.5 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 - hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor Kd = 0.1995 nM 9.7 pA2 for NK2 receptor of rabbit pulmonary artery 16039119
Substance-K receptor IC50 = 3.162 nM 8.5 Inhibition of human Neurokinin 2 receptor 16039119

Literature References

PubMed DOI Target Context # Activities
16039119 10.1016/j.bmcl.2005.05.134 Substance-K receptor 2
16039119 10.1016/j.bmcl.2005.05.134 Homo sapiens 2
16039119 10.1016/j.bmcl.2005.05.134 No relevant target 1

Data from ChEMBL 36 via Core Engine