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Compound Detail

CHEMBL4875667

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CC(=O)N1Cc2cc(S(C)(=O)=O)ccc2C1C(=O)Nc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1

Basic Information

ChEMBL ID CHEMBL4875667
Phase Preclinical
Structure Type MOL
InChI Key QYYZXEPEVBXNNA-UHFFFAOYSA-N
3
Targets
13
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

524.4
MW (Da)
3.44
ALogP
5
HBA
2
HBD
103.8
PSA (Ų)
0.60
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18F6N2O5S
MW 524.44
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.90

Activity Summary

IC50 13 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.22 7.22 60.0 1
Nuclear receptor ROR-gamma
CHEMBL1741186
IC50 7.0 6.4064 100.0 11
Cytochrome P450 2D6
CHEMBL289
IC50 4.92 4.92 12000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 mL.min-1.g-1 Homo sapiens
CL 6.3 mL.min-1.kg-1 Rattus norvegicus
F 40.0 % Rattus norvegicus
T1/2 4.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 60.0 nM 7.22 Suppression of IL-17A production in human Th17 cells incubated for 4 days by IL-... 34464130
Nuclear receptor ROR-gamma IC50 = 100.0 nM 7.0 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Nuclear receptor ROR-gamma IC50 = 106.0 nM 6.97 Inverse agonist activity at human RORC2 assessed as inhibition of SRC1-derived c... 34464130
Nuclear receptor ROR-gamma IC50 = 126.0 nM 6.9 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Nuclear receptor ROR-gamma IC50 = 158.0 nM 6.8 FRET Assay: The assay was run in black 384 well plates (Greiner cat no: 784900).... -
Nuclear receptor ROR-gamma IC50 = 158.0 nM 6.8 FRET Assay: The assay was run in black 384 well plates (Greiner cat no: 784900).... -
Nuclear receptor ROR-gamma IC50 = 631.0 nM 6.2 FRET Assay: The assay was run in black 384 well plates (Greiner cat no: 784900).... -
Nuclear receptor ROR-gamma IC50 = 631.0 nM 6.2 FRET Assay: The assay was run in black 384 well plates (Greiner cat no: 784900).... -
Nuclear receptor ROR-gamma IC50 = 794.0 nM 6.1 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Nuclear receptor ROR-gamma IC50 = 794.0 nM 6.1 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Nuclear receptor ROR-gamma IC50 = 1995.0 nM 5.7 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Nuclear receptor ROR-gamma IC50 = 1995.0 nM 5.7 Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was ... -
Cytochrome P450 2D6 IC50 = 12000.0 nM 4.92 Inhibition of CYP2D6 in human liver microsomes 34464130

Literature References

PubMed DOI Target Context # Activities
34464130 10.1021/acs.jmedchem.1c01197 ADMET 7
34464130 10.1021/acs.jmedchem.1c01197 Nuclear receptor ROR-gamma 1
34464130 10.1021/acs.jmedchem.1c01197 Unchecked 1
34464130 10.1021/acs.jmedchem.1c01197 Voltage-gated inwardly rectifying potassium channel KCNH2 1
34464130 10.1021/acs.jmedchem.1c01197 Cytochrome P450 2D6 1
34464130 10.1021/acs.jmedchem.1c01197 No relevant target 1

Data from ChEMBL 36 via Core Engine