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Compound Detail

CHEMBL4543119

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CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4543119
Phase Preclinical
Structure Type MOL
InChI Key OPBVCSJIFBNFSY-UHFFFAOYSA-N
Parent Compound CHEMBL4596606
Active Moiety CHEMBL4596606
4
Targets
8
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

277.4
MW (Da)
2.08
ALogP
5
HBA
1
HBD
44.3
PSA (Ų)
0.92
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H29F6N5O4
MW 505.46
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -1.74

Activity Summary

EC50 6 meas. best 8.93
Ki 2 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL4468
EC50 8.93 7.705 1.2 2
Histamine H4 receptor
CHEMBL3759
EC50 7.71 7.285 19.5 2
Histamine H4 receptor
CHEMBL5657
EC50 7.45 6.765 35.5 2
Histamine H4 receptor
CHEMBL3759
Ki 7.2 7.2 63.1 1
Histamine H3 receptor
CHEMBL264
Ki 5.62 5.62 2398.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31469288 10.1021/acs.jmedchem.9b01342 Histamine H4 receptor 13
31469288 10.1021/acs.jmedchem.9b01342 Histamine H2 receptor 2
31469288 10.1021/acs.jmedchem.9b01342 Unchecked 2
31469288 10.1021/acs.jmedchem.9b01342 No relevant target 1
31469288 10.1021/acs.jmedchem.9b01342 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine