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Compound Detail

CHEMBL3674077

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Cc1nc2c(c(-c3ccn[nH]3)n1)C[C@@H](C)N(C(=O)c1cccc(C(F)(F)F)c1Cl)C2

Basic Information

ChEMBL ID CHEMBL3674077
Phase Preclinical
Structure Type MOL
InChI Key IKDSIXDWHJJKMA-SNVBAGLBSA-N
4
Targets
21
Activities
3
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

435.8
MW (Da)
4.43
ALogP
4
HBA
1
HBD
74.8
PSA (Ų)
0.65
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 C20H17ClF3N5O
MW 435.84
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.35

Activity Summary

IC50 11 meas. best 8.0
Ki 8 meas. best 8.55
EC50 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL2496
Ki 8.55 8.55 2.8 4
Rattus norvegicus
CHEMBL376
EC50 8.1 8.1 8.0 1
P2X purinoceptor 7
CHEMBL2496
IC50 8.0 7.992 10.0 5
P2X purinoceptor 7
CHEMBL4805
IC50 7.96 7.96 11.0 5
P2X purinoceptor 7
CHEMBL4805
Ki 7.8 7.8 15.8 4
P2X purinoceptor 7
CHEMBL4805
EC50 6.8 6.8 158.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.48 5.48 3300.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 571.0 nM Canis lupus familiaris
F 35.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 Ki = 2.8 nM 8.55 Radioligand binding assay: Human or rat P2X7-1321 N1 cells were collected and fr... -
P2X purinoceptor 7 Ki = 2.8 nM 8.55 Ca2+ flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 2.8 nM 8.55 Ca2+ flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 Ki = 2.8 nM 8.55 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
Rattus norvegicus EC50 = 8.0 nM 8.1 Ex vivo inhibition of P2X7 in po dosed rat measured after 1 to 2 hrs by ARG assa... 27426304
P2X purinoceptor 7 IC50 = 10.0 nM 8.0 Antagonist activity at rat P2X7 receptor expressed in 1321N1 cells assessed as i... 27426304
P2X purinoceptor 7 IC50 = 10.3 nM 7.99 FLIPR Assay: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 ch... -
P2X purinoceptor 7 IC50 = 10.3 nM 7.99 Radioligand Binding Assay: Human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 10.3 nM 7.99 Radioligand Binding Assay: Human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 IC50 = 10.3 nM 7.99 Ca2+ Flux assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 11.1 nM 7.96 Ca2+ flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 11.1 nM 7.96 Ca2+ Flux assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 11.1 nM 7.96 Ca2+ flux Assay: 1321N1 cells expressing the recombinant human or rat P2X7 chann... -
P2X purinoceptor 7 IC50 = 11.0 nM 7.96 Antagonist activity at human recombinant P2X7 receptor expressed in 1321N1 cells... 27426304
P2X purinoceptor 7 IC50 = 11.1 nM 7.96 FLIPR Assay: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 ch... -
P2X purinoceptor 7 Ki = 15.8 nM 7.8 Radioligand Binding Assay: Human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 15.8 nM 7.8 Radioligand binding assay: Human or rat P2X7-1321 N1 cells were collected and fr... -
P2X purinoceptor 7 Ki = 15.8 nM 7.8 Radioligand Binding Assay: Human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 Ki = 15.8 nM 7.8 Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and fro... -
P2X purinoceptor 7 EC50 = 158.0 nM 6.8 Antagonist activity at P2X7 receptor in human whole blood assessed as inhibition... 27426304

Literature References

PubMed DOI Target Context # Activities
27426304 10.1016/j.bmcl.2016.06.048 P2X purinoceptor 7 3
27426304 10.1016/j.bmcl.2016.06.048 ADMET 2
27426304 10.1016/j.bmcl.2016.06.048 Cytochrome P450 3A4 1
27426304 10.1016/j.bmcl.2016.06.048 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine