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Compound Detail

CHEMBL1774461

FLORBETAPIR F 18
💊 Approved Drug
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💊 Approved Drug
CNc1ccc(/C=C/c2ccc(OCCOCCOCC[18F])nc2)cc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1774461
Name FLORBETAPIR F 18
Phase Approved
Structure Type MOL
InChI Key YNDIAUKFXKEXSV-CRYLGTRXSA-N
Parent Compound CHEMBL1908919
Active Moiety CHEMBL1908919

Known Names

(18F)AV-45 18F-AV-45 18f-av45 Amyvid AV-45 F-18 Av45 f-18 Florbetapir (18f) Florbetapir f 18 Florbetapir f-18 Florbetapir(18-f) Florbetapir, f-18
2
Targets
11
Activities
1
Assay Types
0
PK Parameters
20
Publications
11
Known Names
5
Indications
1
Mechanisms

Molecular Properties

360.4
MW (Da)
3.68
ALogP
5
HBA
1
HBD
52.6
PSA (Ų)
0.59
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2012
Availability Prescription
Chirality Achiral

Routes of Administration

Parenteral

Flags

First in Class
USAN Year 2009

Extended Properties

Molecular Formula C20H25FN2O3
MW 359.43
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.94

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Diagnostic agent - - ✓ ✓

Indications

Alzheimer Disease Cognitive Dysfunction Radionuclide Imaging Glioblastoma Multiple Sclerosis

ATC Classification

V09AX05
florbetapir (18F)
Level 1: VARIOUS
Level 2: DIAGNOSTIC RADIOPHARMACEUTICALS

Activity Summary

Ki 11 meas. best 8.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amyloid-beta precursor protein
CHEMBL2487
 Ki 8.54 8.54 2.9 6
Unchecked
CHEMBL612545
 Ki 8.54 8.54 2.9 5

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Amyloid-beta precursor protein Ki = 2.87 nM 8.54 Binding affinity to Beta amyloid aggregates in Alzheimer's disease patient brain... 19845387
Amyloid-beta precursor protein Ki = 2.87 nM 8.54 Binding affinity to amyloid beta aggregates in postmortem human Alzheimer's dise... 24900362
Amyloid-beta precursor protein Ki = 2.87 nM 8.54 Displacement of [18F]-amyvid from amyloid-beta aggregates in alzheimer's disease... 22011144
Amyloid-beta precursor protein Ki = 2.9 nM 8.54 Binding affinity to human amyloid beta plaque 24936237
Unchecked Ki = 2.87 nM 8.54 Binding affinity to beta-amyloid 23047223
Unchecked Ki = 2.9 nM 8.54 Displacement of [125I]IMPY from amyloid beta (1 to 42) after 2 hrs by gamma coun... 23047223
Amyloid-beta precursor protein Ki = 2.87 nM 8.54 Binding affinity to amyloid beta (1-42) aggregates in human Alzheimer's disease ... 22236086
Unchecked Ki = 2.87 nM 8.54 Binding affinity to amyloid beta (1-42) aggregates 22236086
Unchecked Ki = 2.87 nM 8.54 Displacement of [125I]IMPY from amyloid beta (1 to 42) fibrils after 2 hrs by ga... 22690944
Unchecked Ki = 2.87 nM 8.54 Displacement of [125I]-IMPY from amyloid beta (1 to 42) fibrils after 2 hrs by g... 22974116
Amyloid-beta precursor protein Ki = 2.87 nM 8.54 Displacement of [125I]IMPY from amyloid beta in brain homogenate of Alzheimer's ... 23673220

Literature References

PubMed DOI Target Context # Activities
22690944 10.1021/jm300251n Brain 5
22011144 10.1021/jm2009106 Amyloid-beta precursor protein 5
22974116 10.1021/jm300973k Brain 3
22011144 10.1021/jm2009106 Brain 2
24900717 10.1021/ml4000707 Brain 2
22236086 10.1021/jm201400q Brain 2
26435514 10.1016/j.ejmech.2015.09.028 Brain 2
23047223 10.1016/j.ejmech.2012.08.031 Brain 2
23047223 10.1016/j.ejmech.2012.08.031 Unchecked 2
22011144 10.1021/jm2009106 Bone 2
22011144 10.1021/jm2009106 Liver 2
22011144 10.1021/jm2009106 Kidney 2
22011144 10.1021/jm2009106 Muscle 2
22011144 10.1021/jm2009106 Blood 2
24900362 10.1021/ml200123w Brain 2
19845387 10.1021/jm901039z Amyloid-beta precursor protein 1
24936237 10.1021/ml300058m Amyloid-beta precursor protein 1
24900362 10.1021/ml200123w Amyloid-beta precursor protein 1
22236086 10.1021/jm201400q No relevant target 1
21885280 10.1016/j.bmcl.2011.08.003 Brain 1

Data from ChEMBL 36 via Core Engine