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Compound Detail

CHEMBL4865670

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CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1

Basic Information

ChEMBL ID CHEMBL4865670
Phase Preclinical
Structure Type MOL
InChI Key QAMVPRDOVPKGPL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

318.4
MW (Da)
2.24
ALogP
4
HBA
4
HBD
118.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H18N6OS
MW 318.41
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.60

Activity Summary

Ki 1 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL1941
Ki 5.28 5.28 5248.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor Ki = 5248.07 nM 5.28 Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 i... 33548637

Literature References

PubMed DOI Target Context # Activities
33548637 10.1016/j.ejmech.2021.113190 Histamine H2 receptor 5
33548637 10.1016/j.ejmech.2021.113190 Histamine H1 receptor 1
33548637 10.1016/j.ejmech.2021.113190 Histamine H3 receptor 1
33548637 10.1016/j.ejmech.2021.113190 Histamine H4 receptor 1
33548637 10.1016/j.ejmech.2021.113190 Unchecked 1

Data from ChEMBL 36 via Core Engine