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Compound Detail

CHEMBL1202325

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Br.Br.COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1

Basic Information

ChEMBL ID CHEMBL1202325
Phase Preclinical
Structure Type MOL
InChI Key OLSYHXUHRDKJAJ-UHFFFAOYSA-N
Parent Compound CHEMBL561369
Active Moiety CHEMBL561369
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

318.4
MW (Da)
2.85
ALogP
4
HBA
3
HBD
73.8
PSA (Ų)
0.40
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 C16H24Br2N4OS
MW 480.27
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.49

Activity Summary

Ki 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 7.7 7.7 19.9 1
Histamine H4 receptor
CHEMBL3759
Ki 6.8 6.8 158.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19414267 10.1016/j.bmc.2009.04.007 Histamine H4 receptor 2
19414267 10.1016/j.bmc.2009.04.007 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine