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Assay Detail

CHEMBL4381892

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

Binding
Displacement of [3H]PSB-11 from human A3 adenosine receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
Scheeff S, Rivière S, Ruiz J, Abdelrahman A, Schulz-Fincke AC, Köse M, Tiburcy F, Wieczorek H, Gütschow M, Müller CE, Menche D.
J Med Chem (2020) 63 : 1684 -1698
PubMed 31990540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.97 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471610 1 6.21
CHEMBL1784269 ARCHAZOLID F 1 6.07
CHEMBL241106 ARCHAZOLID A 1 6.01
CHEMBL290814 BAFILOMYCIN A1 1 5.97
CHEMBL4593430 1 5.94
CHEMBL411767 ARCHAZOLID B 1 5.93
CHEMBL4447903 1 5.86
CHEMBL4549217 1 5.79
CHEMBL4460252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471610 Ki = 609.0 nM 6.21
CHEMBL1784269 ARCHAZOLID F Ki = 859.0 nM 6.07
CHEMBL241106 ARCHAZOLID A Ki = 967.0 nM 6.01
CHEMBL290814 BAFILOMYCIN A1 Ki = 1080.0 nM 5.97
CHEMBL4593430 Ki = 1140.0 nM 5.94
CHEMBL411767 ARCHAZOLID B Ki = 1180.0 nM 5.93
CHEMBL4447903 Ki = 1376.0 nM 5.86
CHEMBL4549217 Ki = 1611.0 nM 5.79
CHEMBL4460252 Ki >= 10000.0 nM -