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Assay Detail

CHEMBL5129735

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human wild type adenosine A3 receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Expi293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
Shepherd C, Robinson S, Berizzi A, Thompson LEJ, Bird L, Culurgioni S, Varzandeh S, Rawlins PB, Olsen RHJ, Navratilova IH.
ACS Med Chem Lett (2022) 13 : 1172 -1181
PubMed 35859869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 4.36 6.13
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477 ADENOSINE 4.0 1 6.13
CHEMBL485745 GW434756X 1 6.13
CHEMBL5208068 1 4.75
CHEMBL5204663 1 4.72
CHEMBL5184937 1 4.44
CHEMBL47633 1 4.29
CHEMBL143703 1 4.28
CHEMBL4550896 1 4.25
CHEMBL5193059 1 4.10
CHEMBL1417210 1 4.00
CHEMBL5193006 1 3.99
CHEMBL337319 BENZOGUANAMINE 1 3.98
CHEMBL3954022 1 3.80
CHEMBL5195119 1 3.75
CHEMBL1573515 1 3.70
CHEMBL5197070 1 3.40
CHEMBL336555 1 -
CHEMBL5201800 1 -
CHEMBL5197657 1 -
CHEMBL408564 1 -
CHEMBL160333 1 -
CHEMBL63803 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477 ADENOSINE Kd = 740.0 nM 6.13
CHEMBL485745 GW434756X Kd = 740.0 nM 6.13
CHEMBL5208068 Kd = 18000.0 nM 4.75
CHEMBL5204663 Kd = 18900.0 nM 4.72
CHEMBL5184937 Kd = 36500.0 nM 4.44
CHEMBL47633 Kd = 50700.0 nM 4.29
CHEMBL143703 Kd = 52000.0 nM 4.28
CHEMBL4550896 Kd = 56000.0 nM 4.25
CHEMBL5193059 Kd = 80000.0 nM 4.10
CHEMBL1417210 Kd = 101000.0 nM 4.00
CHEMBL5193006 Kd = 102000.0 nM 3.99
CHEMBL337319 BENZOGUANAMINE Kd = 104200.0 nM 3.98
CHEMBL3954022 Kd = 160000.0 nM 3.80
CHEMBL5195119 Kd = 180000.0 nM 3.75
CHEMBL1573515 Kd = 200000.0 nM 3.70
CHEMBL5197070 Kd = 400000.0 nM 3.40
CHEMBL336555 Kd - -
CHEMBL5201800 Kd - -
CHEMBL5197657 Kd - -
CHEMBL408564 Activity - -
CHEMBL160333 Activity - -
CHEMBL63803 Activity - -