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Compound Detail

CHEMBL295252

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CN(C)c1cccc2c(S(=O)(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)cccc12

Basic Information

ChEMBL ID CHEMBL295252
Phase Preclinical
Structure Type MOL
InChI Key QDGYDRMUJVIATQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

591.8
MW (Da)
3.66
ALogP
7
HBA
3
HBD
122.1
PSA (Ų)
0.09
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H41N7O3S
MW 591.78
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.39

Activity Summary

Kd 1 meas. best 5.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL2882
Kd 5.71 5.71 1949.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor Kd = 1949.84 nM 5.71 Histamine H2 receptor antagonistic activity on the isolated spontaneously beatin... 12729649

Literature References

PubMed DOI Target Context # Activities
12729649 10.1016/s0960-894x(03)00235-x Histamine H2 receptor 1

Data from ChEMBL 36 via Core Engine