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Compound Detail

CHEMBL144011

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C=CCC1CCCN(CC2CCN(CCC(/C(COCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)=N/OC)c3ccc(Cl)c(Cl)c3)CC2)C1=O

Basic Information

ChEMBL ID CHEMBL144011
Phase Preclinical
Structure Type MOL
InChI Key BCZOCLLNEUBFJV-CMXZEOLJSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

736.6
MW (Da)
9.25
ALogP
5
HBA
0
HBD
54.4
PSA (Ų)
0.08
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H41Cl2F6N3O3
MW 736.62
Aromatic Rings 2
Heavy Atoms 49
NP-Likeness -0.70

Activity Summary

Ki 2 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 7.89 7.89 13.0 1
Substance-K receptor
CHEMBL2327
Ki 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor Ki = 13.0 nM 7.89 Binding affinity towards NK1 receptor 11229755
Substance-K receptor Ki = 58.0 nM 7.24 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