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Compound Detail

CHEMBL87583

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FC(F)(F)c1cccc(-c2nc(CCNC3CC3)c[nH]2)c1

Basic Information

ChEMBL ID CHEMBL87583
Phase Preclinical
Structure Type MOL
InChI Key CIXJCCIPLDBDFN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

295.3
MW (Da)
3.39
ALogP
2
HBA
2
HBD
40.7
PSA (Ų)
0.89
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H16F3N3
MW 295.31
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -1.39

Activity Summary

Kd 1 meas. best 9.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Kd 9.13 9.13 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor Kd = 0.7413 nM 9.13 Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 ... 9873585

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