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Compound Detail

CHEMBL6056547

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O=C(c1ccnc(C(F)(F)F)c1Cl)N1[C@H]2CCC[C@@H]1c1nnc(-c3ccccn3)n1C2

Basic Information

ChEMBL ID CHEMBL6056547
Phase Preclinical
Structure Type MOL
InChI Key KUKNODUFIBPIAZ-SMDDNHRTSA-N
3
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

448.8
MW (Da)
4.16
ALogP
6
HBA
0
HBD
76.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16ClF3N6O
MW 448.84
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.25

Activity Summary

IC50 6 meas. best 7.9
Ki 6 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL2496
Ki 8.3 8.3 5.0 2
P2X purinoceptor 7
CHEMBL4805
Ki 8.3 7.8333 5.0 3
P2X purinoceptor 7
CHEMBL5183
Ki 8.3 8.3 5.0 1
P2X purinoceptor 7
CHEMBL5183
IC50 7.9 7.9 12.7 1
P2X purinoceptor 7
CHEMBL2496
IC50 7.89 7.19 13.0 2
P2X purinoceptor 7
CHEMBL4805
IC50 7.53 7.18 29.5 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 Ki = 5.0 nM 8.3 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 5.0 nM 8.3 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 5.0 nM 8.3 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 5.0 nM 8.3 P2X7 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected an... -
P2X purinoceptor 7 IC50 = 12.7 nM 7.9 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -
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 Ki = 25.0 nM 7.6 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 25.1 nM 7.6 P2X7 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected an... -
P2X purinoceptor 7 IC50 = 29.5 nM 7.53 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -
P2X purinoceptor 7 IC50 = 30.0 nM 7.52 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 327.0 nM 6.49 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 327.0 nM 6.49 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -

Data from ChEMBL 36 via Core Engine