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Compound Detail

CHEMBL3697520

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O=C(c1cccc(C(F)(F)F)c1Cl)N1[C@H]2CCC[C@@H]1c1nnc(-c3cccnc3)n1C2

Basic Information

ChEMBL ID CHEMBL3697520
Phase Preclinical
Structure Type MOL
InChI Key HIHBQMZMGKEOHM-XJKSGUPXSA-N
3
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

447.9
MW (Da)
4.76
ALogP
5
HBA
0
HBD
63.9
PSA (Ų)
0.57
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17ClF3N5O
MW 447.85
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.42

Activity Summary

IC50 7 meas. best 8.09
Ki 5 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL2496
IC50 8.09 8.09 8.2 2
P2X purinoceptor 7
CHEMBL5183
IC50 8.09 8.09 8.2 1
P2X purinoceptor 7
CHEMBL4805
IC50 8.0 7.8575 10.0 4
P2X purinoceptor 7
CHEMBL2496
Ki 7.77 7.77 17.0 1
P2X purinoceptor 7
CHEMBL4805
Ki 7.77 7.765 17.0 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 IC50 = 8.2 nM 8.09 FLIPR Assay: Ca.sup.2+flux: 1321N1 cells expressing the recombinant human, rat o... -
P2X purinoceptor 7 IC50 = 8.2 nM 8.09 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 8.2 nM 8.09 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -
P2X purinoceptor 7 IC50 = 10.0 nM 8.0 FLIPR Assay: Ca.sup.2+flux: 1321N1 cells expressing the recombinant human, rat o... -
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 = 10.0 nM 8.0 P2X7 FLIPR Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chan... -
P2X purinoceptor 7 Ki = 17.0 nM 7.77 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 17.0 nM 7.77 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 17.0 nM 7.77 Ca2+ Flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 17.4 nM 7.76 Radioligand Binding: Human or rat P2X7-1321N1 cells were collected and frozen @-... -
P2X purinoceptor 7 Ki = 17.4 nM 7.76 P2X7 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected an... -
P2X purinoceptor 7 IC50 = 37.0 nM 7.43 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -

Data from ChEMBL 36 via Core Engine