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Compound Detail

CHEMBL34327

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COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL34327
Phase Preclinical
Structure Type MOL
InChI Key NCLGVWVXAVALGO-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
3.38
ALogP
3
HBA
1
HBD
43.3
PSA (Ų)
0.76
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 C20H22N2O2
MW 322.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.12

Activity Summary

Ki 5 meas. best 8.19
IC50 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 8.19 8.19 6.5 2
Melatonin receptor type 1A
CHEMBL1945
Ki 6.85 6.85 141.2 2
Melatonin receptor
CHEMBL2094268
Ki 6.54 6.54 287.0 1
Melatonin receptor
CHEMBL2094268
IC50 5.96 5.96 1090.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9748358 10.1021/jm9810093 Melatonin receptor 3
12672242 10.1021/jm020982d Melatonin receptor type 1A 3
12672242 10.1021/jm020982d Melatonin receptor type 1B 3
9748358 10.1021/jm9810093 Melatonin receptor type 1C 1
15943478 10.1021/jm048956y Melatonin receptor type 1A 1
15943478 10.1021/jm048956y Melatonin receptor type 1B 1

Data from ChEMBL 36 via Core Engine