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Compound Detail

CHEMBL5424175

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Brc1ccc2[nH]nc(C3=CCCNC3)c2c1

Basic Information

ChEMBL ID CHEMBL5424175
Phase Preclinical
Structure Type MOL
InChI Key OZAHEVLLVSEENQ-UHFFFAOYSA-N
3
Targets
7
Activities
2
Assay Types
8
PK Parameters
4
Publications
0
Known Names

Molecular Properties

278.1
MW (Da)
2.70
ALogP
2
HBA
2
HBD
40.7
PSA (Ų)
0.84
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H12BrN3
MW 278.15
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -0.42

Activity Summary

EC50 6 meas. best 8.25
IC50 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 8.25 8.05 5.6 2
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 7.82 7.82 15.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.24 7.235 58.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 6.72 6.72 189.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 5.6 mL.min-1.kg-1 Homo sapiens
CL 58.0 mL.min-1.kg-1 Rattus norvegicus
CL 57.0 mL.min-1.kg-1 Mus musculus
CL 34.2 mL.min-1.kg-1 Rattus norvegicus
Fu 0.12 - Homo sapiens
Fu 0.13 - Rattus norvegicus
Fu 0.12 - Mus musculus
T1/2 2.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38352850 10.1021/acsmedchemlett.3c00566 ADMET 12
38352850 10.1021/acsmedchemlett.3c00566 5-hydroxytryptamine receptor 2A 4
38352850 10.1021/acsmedchemlett.3c00566 5-hydroxytryptamine receptor 2B 3
38352850 10.1021/acsmedchemlett.3c00566 5-hydroxytryptamine receptor 2C 3

Data from ChEMBL 36 via Core Engine