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Compound Detail

CHEMBL130354

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

Basic Information

ChEMBL ID CHEMBL130354
Phase Preclinical
Structure Type MOL
InChI Key QKDREOIGKWPZQZ-RRYCAANRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

783.7
MW (Da)
9.03
ALogP
7
HBA
1
HBD
75.6
PSA (Ų)
0.12
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 C36H46Cl2F6N4O4
MW 783.68
Aromatic Rings 2
Heavy Atoms 52
NP-Likeness -0.93

Activity Summary

Ki 2 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 7.77 7.77 17.0 1
Substance-K receptor
CHEMBL2327
Ki 7.48 7.48 33.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor Ki = 17.0 nM 7.77 Binding affinity towards NK1 receptor 11229755
Substance-K receptor Ki = 33.0 nM 7.48 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