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Compound Detail

CHEMBL5558681

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O=C(O)c1ccc(CCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1

Basic Information

ChEMBL ID CHEMBL5558681
Phase Preclinical
Structure Type MOL
InChI Key CSTPKAXJLQELNB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

473.0
MW (Da)
6.06
ALogP
3
HBA
1
HBD
53.4
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29ClN2O2
MW 473.02
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 7.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
IC50 7.19 7.19 64.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 64.51 nM 7.19 Antagonist activity at human H1 receptor expressed in PathHunter CHO-K1 HRH1 bet... 38368709

Literature References

PubMed DOI Target Context # Activities
38368709 10.1016/j.ejmech.2024.116197 Histamine H1 receptor 1
38368709 10.1016/j.ejmech.2024.116197 Muscarinic acetylcholine receptor M3 1
38368709 10.1016/j.ejmech.2024.116197 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine