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Compound Detail

CHEMBL109514

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Fc1ccc(C(COCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N2CCNCC2)cc1

Basic Information

ChEMBL ID CHEMBL109514
Phase Preclinical
Structure Type MOL
InChI Key LEPMWVSFBIGRRP-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

450.4
MW (Da)
5.03
ALogP
3
HBA
1
HBD
24.5
PSA (Ų)
0.63
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21F7N2O
MW 450.40
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 7.0
Ki 1 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 7.1 7.1 79.4 1
Substance-P receptor
CHEMBL249
IC50 7.0 7.0 100.0 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 6.8 6.8 158.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12565946 10.1016/s0960-894x(02)00956-3 Substance-P receptor 1
12372532 10.1016/s0960-894x(02)00563-2 Substance-P receptor 1
12372532 10.1016/s0960-894x(02)00563-2 Sodium-dependent serotonin transporter 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine