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Compound Detail

CHEMBL11001

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CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(Br)cnc32)CC1

Basic Information

ChEMBL ID CHEMBL11001
Phase Preclinical
Structure Type MOL
InChI Key YTBOCPITYZKISK-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

431.8
MW (Da)
5.04
ALogP
2
HBA
0
HBD
33.2
PSA (Ų)
0.59
QED
1
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20BrClN2O
MW 431.76
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 5.64
Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL4701
Ki 8.0 8.0 10.0 1
Homo sapiens
CHEMBL372
IC50 5.64 5.64 2290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(00)80290-5 Homo sapiens 1
- 10.1016/S0960-894X(00)80290-5 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine