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Compound Detail

CHEMBL89245

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O=C(CCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(c1ccc(F)cc1)C1CCNCC1

Basic Information

ChEMBL ID CHEMBL89245
Phase Preclinical
Structure Type MOL
InChI Key DORXFPYAVMERKG-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.4
MW (Da)
5.58
ALogP
2
HBA
1
HBD
32.3
PSA (Ų)
0.59
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21F7N2O
MW 462.41
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 6.7
Ki 2 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 6.7 6.7 199.5 1
Substance-P receptor
CHEMBL249
Ki 6.7 6.7 199.5 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.6 6.6 251.2 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 6.6 6.6 251.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11755367 10.1016/s0960-894x(01)00727-2 Substance-P receptor 1
11755367 10.1016/s0960-894x(01)00727-2 Sodium-dependent serotonin transporter 1
11755367 10.1016/s0960-894x(01)00727-2 No relevant target 1
16220969 10.1021/jm058225d Substance-P receptor 1
16220969 10.1021/jm058225d Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine