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Compound Detail

CHEMBL5201470

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Cl.Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1

Basic Information

ChEMBL ID CHEMBL5201470
Phase Preclinical
Structure Type MOL
InChI Key QXYJMCLXSJHKBZ-UHFFFAOYSA-N
Parent Compound CHEMBL5222574
Active Moiety CHEMBL5222574
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

298.3
MW (Da)
2.95
ALogP
3
HBA
4
HBD
68.3
PSA (Ų)
0.52
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H16ClFN2O2
MW 334.78
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness 0.41

Activity Summary

EC50 6 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.6 7.6 25.0 2
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.38 7.38 41.7 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 7.14 7.14 72.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35450369 10.1021/acsmedchemlett.1c00694 5-hydroxytryptamine receptor 2A 3
35450369 10.1021/acsmedchemlett.1c00694 5-hydroxytryptamine receptor 2C 3
35450369 10.1021/acsmedchemlett.1c00694 5-hydroxytryptamine receptor 2B 3
35450369 10.1021/acsmedchemlett.1c00694 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1

Data from ChEMBL 36 via Core Engine