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Compound Detail

CHEMBL182937

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C[C@H](Nc1nc(N)nc(NCCOc2ccc(F)cc2)n1)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL182937
Phase Preclinical
Structure Type MOL
InChI Key UNUSDSJWMRJMCT-LBPRGKRZSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

386.4
MW (Da)
3.40
ALogP
7
HBA
3
HBD
98.0
PSA (Ų)
0.51
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20F2N6O
MW 386.41
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.36

Activity Summary

Ki 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 8.7 8.7 2.0 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 57.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15261279 10.1016/j.bmcl.2004.06.008 5-hydroxytryptamine receptor 7 1
15261279 10.1016/j.bmcl.2004.06.008 Rattus norvegicus 1
15261279 10.1016/j.bmcl.2004.06.008 5-hydroxytryptamine receptor 6 1
15261279 10.1016/j.bmcl.2004.06.008 Adrenergic receptor alpha-1 1
15261279 10.1016/j.bmcl.2004.06.008 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine