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Assay Detail

CHEMBL5735451

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Binding
Fluorescent Displacement Assay: A Nunc black plate was used as a 96-well plate for the purpose of measurement, and to each well was added 40 μL of sodium phosphate buffer and a sodium phosphate buffer solution of FABP3 (AVISCERA BIOSCIENCE) (250 nM, 25 μL), and for a blank, 25 μL of sodium phosphate buffer was added. To each well was added as a detection reagent, a 1,8-ANS (ALDRICH) solution (10 μM, ethanol/sodium phosphate buffer solution=1:4 v/v, 25 μL), and ethanol solutions of compounds diluted to different concentrations were added in an amount of 10 μL each (the final ethanol concentration was 15%). The plate was shaken for 10 sec. in the plate reader and incubated for 10 min. at room temperature. Then, it was subjected to fluorescent measurement at an excitation wavelength of 355 nm and a measurement wavelength of 460 nm. Used for measurement was ARVO X One by PerkinElmer Japan.
60
Total Activities
16
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty acid-binding protein, heart (CHEMBL3344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Agent for treating synucleinopathy
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
kon 20 - -
k_off 20 - -
IC50 10 6.36 7.28
Kd 10 5.89 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5878164 3 7.28
CHEMBL5555714 6 7.11
CHEMBL5770423 6 6.55
CHEMBL5976044 3 6.38
CHEMBL6048509 3 6.29
CHEMBL2334261 3 6.16
CHEMBL2334255 6 6.14
CHEMBL2334257 3 6.10
CHEMBL5777988 3 6.10
CHEMBL5757642 3 6.01
CHEMBL5567823 3 5.95
CHEMBL5801911 3 5.89
CHEMBL5753881 3 5.89
CHEMBL2334254 3 5.70
CHEMBL5754165 3 5.55
CHEMBL2334260 6 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5878164 IC50 = 52.0 nM 7.28
CHEMBL5555714 IC50 = 77.0 nM 7.11
CHEMBL5770423 IC50 = 280.0 nM 6.55
CHEMBL5555714 Kd = 386.0 nM 6.41
CHEMBL5976044 Kd = 414.0 nM 6.38
CHEMBL6048509 IC50 = 510.0 nM 6.29
CHEMBL2334261 IC50 = 700.0 nM 6.16
CHEMBL2334255 IC50 = 730.0 nM 6.14
CHEMBL2334257 IC50 = 790.0 nM 6.10
CHEMBL5777988 Kd = 787.0 nM 6.10
CHEMBL5757642 Kd = 968.0 nM 6.01
CHEMBL5567823 Kd = 1128.0 nM 5.95
CHEMBL2334255 Kd = 1246.0 nM 5.90
CHEMBL5753881 Kd = 1293.0 nM 5.89
CHEMBL5801911 IC50 = 1300.0 nM 5.89
CHEMBL2334254 IC50 = 2000.0 nM 5.70
CHEMBL5770423 Kd = 2216.0 nM 5.65
CHEMBL5754165 Kd = 2846.0 nM 5.55
CHEMBL2334260 Kd = 9625.0 nM 5.02
CHEMBL2334254 k_off = - s-1 -
CHEMBL2334255 k_off = - s-1 -
CHEMBL2334261 k_off = - s-1 -
CHEMBL2334261 kon = - -
CHEMBL2334257 k_off = - s-1 -
CHEMBL2334257 kon = - -
CHEMBL5878164 k_off = - s-1 -
CHEMBL5878164 kon = - -
CHEMBL5770423 k_off = - s-1 -
CHEMBL5770423 kon = - -
CHEMBL2334255 k_off = - s-1 -
CHEMBL2334255 kon = - -
CHEMBL5555714 k_off = - s-1 -
CHEMBL5555714 kon = - -
CHEMBL2334254 kon = - -
CHEMBL5976044 kon = - -
CHEMBL5567823 k_off = - s-1 -
CHEMBL5567823 kon = - -
CHEMBL5976044 k_off = - s-1 -
CHEMBL5777988 kon = - -
CHEMBL5757642 k_off = - s-1 -
CHEMBL5777988 k_off = - s-1 -
CHEMBL5757642 kon = - -
CHEMBL2334260 k_off = - s-1 -
CHEMBL2334260 kon = - -
CHEMBL5753881 kon = - -
CHEMBL5770423 k_off = - s-1 -
CHEMBL5770423 kon = - -
CHEMBL5754165 kon = - -
CHEMBL5753881 k_off = - s-1 -
CHEMBL5754165 k_off = - s-1 -