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Compound Detail

CHEMBL314947

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COc1ccc2oc(Cc3cccc(C(F)(F)F)c3)c(CCNC(C)=O)c2c1

Basic Information

ChEMBL ID CHEMBL314947
Phase Preclinical
Structure Type MOL
InChI Key QZNYRKGPXRZKKE-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

391.4
MW (Da)
4.73
ALogP
3
HBA
1
HBD
51.5
PSA (Ų)
0.66
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20F3NO3
MW 391.39
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.64

Activity Summary

Ki 2 meas. best 8.93
EC50 1 meas. best 8.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 8.93 8.93 1.2 1
Melatonin receptor type 1B
CHEMBL1946
EC50 8.9 8.9 1.3 1
Melatonin receptor type 1A
CHEMBL1945
Ki 7.1 7.1 80.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12061881 10.1021/jm0005252 Melatonin receptor type 1A 4
12061881 10.1021/jm0005252 Melatonin receptor type 1B 4
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor type 1A 1
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor type 1B 1
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor 1
12061881 10.1021/jm0005252 Melatonin receptor 1

Data from ChEMBL 36 via Core Engine