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Compound Detail

CHEMBL148282

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CO/N=C(\COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(CN2CCCC(O)C2)CC1)c1ccc(Cl)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL148282
Phase Preclinical
Structure Type MOL
InChI Key PNFHNRJQQVSHOG-AETRBLLXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

698.6
MW (Da)
7.89
ALogP
6
HBA
1
HBD
57.5
PSA (Ų)
0.14
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39Cl2F6N3O3
MW 698.58
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.91

Activity Summary

Ki 2 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 7.42 7.42 38.0 1
Substance-K receptor
CHEMBL2327
Ki 7.33 7.33 47.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor Ki = 38.0 nM 7.42 Binding affinity towards NK1 receptor 11229755
Substance-K receptor Ki = 47.0 nM 7.33 Binding affinity towards NK2 receptor 11229755

Literature References

PubMed DOI Target Context # Activities
11229755 10.1016/s0960-894x(00)00702-2 Substance-P receptor 1
11229755 10.1016/s0960-894x(00)00702-2 Substance-K receptor 1

Data from ChEMBL 36 via Core Engine