Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4406029

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

Binding
Displacement of [125I]I-AB-MECA from recombinant mouse A3AR expressed in HEK293 cell membranes measured after 60 mins by liquid scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL1075269)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution.
Tosh DK, Salmaso V, Rao H, Bitant A, Fisher CL, Lieberman DI, Vorbrüggen H, Reitman ML, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA.
J Med Chem (2020) 63 : 4334 -4348
PubMed 32271569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.78 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4571380 1 7.75
CHEMBL4465891 1 7.67
CHEMBL4483546 1 7.58
CHEMBL4556534 1 7.40
CHEMBL4442223 1 7.26
CHEMBL4561796 1 7.22
CHEMBL4456051 1 7.21
CHEMBL4573502 1 7.14
CHEMBL4476812 1 7.13
CHEMBL4459700 1 7.12
CHEMBL4459684 1 7.12
CHEMBL4455589 1 7.03
CHEMBL4591186 1 6.91
CHEMBL4438591 1 6.81
CHEMBL4562690 1 6.58
CHEMBL4453175 1 6.48
CHEMBL4437771 1 6.39
CHEMBL2089346 1 6.32
CHEMBL4519265 1 6.31
CHEMBL4537118 1 6.28
CHEMBL4550711 1 6.17
CHEMBL2089347 1 6.01
CHEMBL4475372 1 6.00
CHEMBL4448826 1 5.94
CHEMBL4521342 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4571380 Ki = 17.8 nM 7.75
CHEMBL4465891 Ki = 21.5 nM 7.67
CHEMBL4483546 Ki = 26.0 nM 7.58
CHEMBL4556534 Ki = 39.8 nM 7.40
CHEMBL4442223 Ki = 54.4 nM 7.26
CHEMBL4561796 Ki = 60.4 nM 7.22
CHEMBL4456051 Ki = 61.6 nM 7.21
CHEMBL4573502 Ki = 72.2 nM 7.14
CHEMBL4476812 Ki = 74.7 nM 7.13
CHEMBL4459700 Ki = 76.4 nM 7.12
CHEMBL4459684 Ki = 75.0 nM 7.12
CHEMBL4455589 Ki = 92.5 nM 7.03
CHEMBL4591186 Ki = 122.0 nM 6.91
CHEMBL4438591 Ki = 155.0 nM 6.81
CHEMBL4562690 Ki = 264.0 nM 6.58
CHEMBL4453175 Ki = 331.0 nM 6.48
CHEMBL4437771 Ki = 404.0 nM 6.39
CHEMBL2089346 Ki = 480.0 nM 6.32
CHEMBL4519265 Ki = 488.0 nM 6.31
CHEMBL4537118 Ki = 531.0 nM 6.28
CHEMBL4550711 Ki = 675.0 nM 6.17
CHEMBL2089347 Ki = 980.0 nM 6.01
CHEMBL4475372 Ki = 995.0 nM 6.00
CHEMBL4448826 Ki = 1140.0 nM 5.94
CHEMBL4521342 Ki = 2520.0 nM 5.60