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Compound Detail

CHEMBL314438

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CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1

Basic Information

ChEMBL ID CHEMBL314438
Phase Preclinical
Structure Type MOL
InChI Key GOHPIKDATUAMSC-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

283.3
MW (Da)
3.20
ALogP
2
HBA
1
HBD
31.9
PSA (Ų)
0.93
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H16F3N3
MW 283.30
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -1.37

Activity Summary

Kd 4 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Kd 8.92 8.885 1.2 2
Histamine H3 receptor
CHEMBL5076
Kd 5.95 5.95 1122.0 1
Muscarinic acetylcholine receptor M3
CHEMBL5498
Kd 4.57 4.57 26915.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9873585 10.1016/s0960-894x(98)00461-2 Histamine H1 receptor 9
9873585 10.1016/s0960-894x(98)00461-2 Histamine H2 receptor 1
9873585 10.1016/s0960-894x(98)00461-2 Histamine H3 receptor 1
9873585 10.1016/s0960-894x(98)00461-2 Muscarinic acetylcholine receptor M3 1

Data from ChEMBL 36 via Core Engine