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Compound Detail

CHEMBL6023464

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O=C(c1ccc(F)c(C(F)(F)F)c1Cl)N1[C@H]2CCC[C@@H]1c1nnc(-c3ccccn3)n1C2

Basic Information

ChEMBL ID CHEMBL6023464
Phase Preclinical
Structure Type MOL
InChI Key PTQTUXJAFONBHH-XHDPSFHLSA-N
3
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

465.8
MW (Da)
4.90
ALogP
5
HBA
0
HBD
63.9
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16ClF4N5O
MW 465.84
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.30

Activity Summary

IC50 6 meas. best 8.0
Ki 6 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL2496
Ki 8.49 8.49 3.2 2
P2X purinoceptor 7
CHEMBL4805
Ki 8.49 8.14 3.2 3
P2X purinoceptor 7
CHEMBL5183
Ki 8.49 8.49 3.2 1
P2X purinoceptor 7
CHEMBL2496
IC50 8.0 7.945 10.0 2
P2X purinoceptor 7
CHEMBL5183
IC50 7.99 7.99 10.2 1
P2X purinoceptor 7
CHEMBL4805
IC50 7.89 7.8833 13.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 Ki = 3.2 nM 8.49 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 3.2 nM 8.49 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 3.2 nM 8.49 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 3.2 nM 8.49 P2X7 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected an... -
P2X purinoceptor 7 IC50 = 10.0 nM 8.0 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 10.2 nM 7.99 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -
P2X purinoceptor 7 Ki = 10.7 nM 7.97 P2X7 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected an... -
P2X purinoceptor 7 Ki = 11.0 nM 7.96 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 13.0 nM 7.89 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 13.0 nM 7.89 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 13.0 nM 7.89 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 13.4 nM 7.87 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -

Data from ChEMBL 36 via Core Engine