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Compound Detail

CHEMBL139499

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NC(=O)CN1CCN([C@@H](COCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL139499
Phase Preclinical
Structure Type MOL
InChI Key SQNYJTSIWKBHBD-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

489.5
MW (Da)
4.09
ALogP
4
HBA
1
HBD
58.8
PSA (Ų)
0.57
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25F6N3O2
MW 489.46
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.31

Activity Summary

Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 50.0 mL.min-1.g-1 -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine