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Compound Detail

CHEMBL14469

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COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cccnc3)c1)CC2

Basic Information

ChEMBL ID CHEMBL14469
Phase Preclinical
Structure Type MOL
InChI Key QODRLEBXZLZSBQ-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

447.8
MW (Da)
6.02
ALogP
3
HBA
1
HBD
54.5
PSA (Ų)
0.53
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H17ClF3N3O2
MW 447.84
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.55

Activity Summary

Ki 3 meas. best 8.3
IC50 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 8.3 8.3 5.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 7.6 7.6 25.1 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.9 5.9 1258.9 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.14 4.14 73000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2A 1
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2B 1
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2C 1
10737744 10.1021/jm990388c Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
10737744 10.1021/jm990388c Serotonin receptor (2b and 2c) 1
10737744 10.1021/jm990388c Cytochrome P450 1A2 1
10737744 10.1021/jm990388c Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine