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Compound Detail

CHEMBL4538671

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CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4538671
Phase Preclinical
Structure Type MOL
InChI Key BKFNRYCNSLJHDB-UTONKHPSSA-N
Parent Compound CHEMBL4595399
Active Moiety CHEMBL4595399
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

305.4
MW (Da)
2.04
ALogP
5
HBA
2
HBD
70.2
PSA (Ų)
0.87
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H28F3N5O3
MW 419.45
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -1.89

Activity Summary

Ki 3 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL3759
Ki 5.58 5.58 2630.3 1
Histamine H3 receptor
CHEMBL264
Ki 5.52 5.52 3019.9 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31469288 10.1021/acs.jmedchem.9b01342 Histamine H3 receptor 2
31469288 10.1021/acs.jmedchem.9b01342 Histamine H2 receptor 2
31469288 10.1021/acs.jmedchem.9b01342 Unchecked 2
31469288 10.1021/acs.jmedchem.9b01342 Histamine H4 receptor 1

Data from ChEMBL 36 via Core Engine