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Compound Detail

CHEMBL5951677

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CC(O)C(C)Oc1cc(C(=O)N[C@H](C)c2cnc(C(F)(F)F)nc2)cc(-c2ncc(Cl)s2)c1

Basic Information

ChEMBL ID CHEMBL5951677
Phase Preclinical
Structure Type MOL
InChI Key QTLJKKFADUZLKR-VOMCLLRMSA-N
4
Targets
34
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

500.9
MW (Da)
4.91
ALogP
7
HBA
2
HBD
97.2
PSA (Ų)
0.48
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20ClF3N4O3S
MW 500.93
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.10

Activity Summary

IC50 34 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 8.4 8.2675 4.0 16
P2X purinoceptor 2
CHEMBL2531
IC50 6.91 6.8125 123.0 8
P2X2/P2X3 heterotrimeric receptor
CHEMBL3831281
IC50 6.91 6.8125 123.0 8
Cytochrome P450 2C8
CHEMBL3721
IC50 4.72 4.72 19000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 4.0 nM 8.4 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 4.0 nM 8.4 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 4.0 nM 8.4 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X purinoceptor 3 IC50 = 4.0 nM 8.4 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 3 IC50 = 5.0 nM 8.3 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 5.0 nM 8.3 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 5.0 nM 8.3 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 3 IC50 = 5.0 nM 8.3 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X purinoceptor 3 IC50 = 6.0 nM 8.22 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 6.0 nM 8.22 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 6.0 nM 8.22 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 3 IC50 = 6.0 nM 8.22 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X purinoceptor 3 IC50 = 7.0 nM 8.15 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 7.0 nM 8.15 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 7.0 nM 8.15 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 3 IC50 = 7.0 nM 8.15 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X2/P2X3 heterotrimeric receptor IC50 = 123.0 nM 6.91 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X purinoceptor 2 IC50 = 123.0 nM 6.91 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X2/P2X3 heterotrimeric receptor IC50 = 123.0 nM 6.91 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 2 IC50 = 123.0 nM 6.91 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -

Data from ChEMBL 36 via Core Engine