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Compound Detail

CHEMBL1475693

FAMPROFAZONE
🧪 Phase II
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🧪 Phase II
CC(C)c1c(CN(C)C(C)Cc2ccccc2)n(C)n(-c2ccccc2)c1=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1475693
Name FAMPROFAZONE
Phase Phase II
Structure Type MOL
InChI Key GNUXVOXXWGNPIV-UHFFFAOYSA-N

Known Names

Famprofazona Famprofazone NSC-759244
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
3
Known Names

Molecular Properties

377.5
MW (Da)
4.36
ALogP
4
HBA
0
HBD
30.2
PSA (Ų)
0.61
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Flags

Natural Product

Extended Properties

Molecular Formula C24H31N3O
MW 377.53
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.79

Activity Summary

EC50 6 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
 EC50 6.89 5.886 130.0 5
Nuclear receptor subfamily 1 group I member 2
CHEMBL2146315
 EC50 5.01 5.01 9800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nuclear receptor subfamily 1 group I member 2 EC50 = 130.0 nM 6.89 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Nuclear receptor subfamily 1 group I member 2 EC50 = 1300.0 nM 5.89 Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 1400.0 nM 5.85 Activation of PXR in human cryopreserved hepatocytes assessed as induction of CY... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 3100.0 nM 5.51 Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induc... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 5100.0 nM 5.29 Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by l... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 9800.0 nM 5.01 Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase ... 20966043

Literature References

PubMed DOI Target Context # Activities
- 10.5281/zenodo.13943903 ADMET 89
31158845 10.1038/s41586-019-1291-3 ADMET 75
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 9
- 10.6019/CHEMBL5724696 TERT-RPE1 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL5665443 DNA-3-methyladenine glycosylase 1
- 10.6019/CHEMBL5665443 Uracil-DNA glycosylase 1
- 10.6019/CHEMBL5665443 G/T mismatch-specific thymine DNA glycosylase 1
- 10.6019/CHEMBL5665443 Single-strand selective monofunctional uracil DNA glycosylase 1
- 10.6019/CHEMBL5665443 N-glycosylase/DNA lyase 1
- 10.6019/CHEMBL5665443 Endonuclease III-like protein 1 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 2 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 1 1
- 10.6019/CHEMBL5665443 Adenine DNA glycosylase 1
- 10.6019/CHEMBL5665443 Methyl-CpG-binding domain protein 4 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine