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Compound Detail

CHEMBL4537738

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O=C(Cc1ccccc1[N+](=O)[O-])Nc1ccc(-c2ccc(C(O)(C(F)(F)F)C(F)(F)F)cc2F)cc1

Basic Information

ChEMBL ID CHEMBL4537738
Phase Preclinical
Structure Type MOL
InChI Key MNVXADPCMINSEC-UHFFFAOYSA-N
7
Targets
9
Activities
2
Assay Types
11
PK Parameters
20
Publications
0
Known Names

Molecular Properties

516.4
MW (Da)
5.89
ALogP
4
HBA
2
HBD
92.5
PSA (Ų)
0.24
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H15F7N2O4
MW 516.37
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.23

Activity Summary

IC50 8 meas. best 6.72
Kd 1 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor ROR-gamma
CHEMBL1741186
IC50 6.72 6.09 190.0 2
Nuclear receptor ROR-gamma
CHEMBL1741186
Kd 6.11 6.11 780.0 1
LNCaP
CHEMBL612518
IC50 5.29 5.29 5140.0 1
Nuclear receptor ROR-alpha
CHEMBL5868
IC50 5.12 5.12 7570.0 1
CWR22R
CHEMBL612657
IC50 5.05 5.05 9000.0 1
LNCaP C4-2B
CHEMBL4296461
IC50 5.04 5.04 9200.0 1
PC-3
CHEMBL390
IC50 4.95 4.95 11140.0 1
DU-145
CHEMBL613508
IC50 4.55 4.55 28430.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3335.0 ng.hr.mL-1 Rattus norvegicus
AUC 6444.0 ng.hr.mL-1 Rattus norvegicus
AUC 3217.0 ng.hr.mL-1 Rattus norvegicus
CL 5.445 mL.min-1.kg-1 Rattus norvegicus
Cmax 1624.8 nM Rattus norvegicus
Cmax 1396.29 nM Rattus norvegicus
F 19.0 % Rattus norvegicus
T1/2 7.67 hr Rattus norvegicus
Tmax 0.19 hr Rattus norvegicus
Tmax 8.0 hr Rattus norvegicus
Vz 3425.0 mg kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30964293 10.1021/acs.jmedchem.9b00327 ADMET 12
- 10.6019/CHEMBL5303304 HEK-293T 10
- 10.6019/CHEMBL5303304 Fibroblast 8
30964293 10.1021/acs.jmedchem.9b00327 Nuclear receptor ROR-gamma 4
- 10.6019/CHEMBL5303304 U2OS 4
30964293 10.1021/acs.jmedchem.9b00327 Nuclear receptor ROR-alpha 2
30964293 10.1021/acs.jmedchem.9b00327 CWR22R 1
30964293 10.1021/acs.jmedchem.9b00327 LNCaP C4-2B 1
30964293 10.1021/acs.jmedchem.9b00327 DU-145 1
30964293 10.1021/acs.jmedchem.9b00327 PC-3 1
30964293 10.1021/acs.jmedchem.9b00327 LNCaP 1
30964293 10.1021/acs.jmedchem.9b00327 Bile acid receptor 1
30964293 10.1021/acs.jmedchem.9b00327 Oxysterols receptor LXR-alpha 1
30964293 10.1021/acs.jmedchem.9b00327 Nuclear receptor ROR-beta 1
- 10.6019/CHEMBL5308504 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5308504 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5308504 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5308504 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5308504 Aurora kinase A 1
- 10.6019/CHEMBL5308504 Tyrosine-protein kinase ABL1 1

Data from ChEMBL 36 via Core Engine