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Compound Detail

CHEMBL136850

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COc1cc(CN2CCN(C(COCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccccc3)C(Cc3ccccc3)C2)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL136850
Phase Preclinical
Structure Type MOL
InChI Key ONJMXWFIKVVLCT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

702.7
MW (Da)
8.44
ALogP
6
HBA
0
HBD
43.4
PSA (Ų)
0.13
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H40F6N2O4
MW 702.74
Aromatic Rings 4
Heavy Atoms 50
NP-Likeness -0.68

Activity Summary

Ki 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 6.6 6.6 251.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor Ki = 251.19 nM 6.6 Displacement of [3H]-substance P from human NK1 receptor expressed in CHO cells 12565946

Literature References

PubMed DOI Target Context # Activities
12565946 10.1016/s0960-894x(02)00956-3 No relevant target 2
12565946 10.1016/s0960-894x(02)00956-3 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine