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Assay Detail

CHEMBL901888

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

Binding
Displacement of [3H]CPX from adenosine A1 receptor expressed in DDT1 MF2 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type DDT1 MF2
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of adenosines with heterocyclic N6-substituents.
Ashton TD, Aumann KM, Baker SP, Schiesser CH, Scammells PJ.
Bioorg Med Chem Lett (2007) 17 : 6779 -6784
PubMed 17967536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.95 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240065 1 8.10
CHEMBL430374 1 7.68
CHEMBL240279 1 7.50
CHEMBL391031 1 7.29
CHEMBL392149 TECADENOSON 2.0 1 7.19
CHEMBL391029 1 7.16
CHEMBL240487 1 6.79
CHEMBL240278 1 6.54
CHEMBL392720 1 6.11
CHEMBL391030 1 6.09
CHEMBL240277 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240065 Ki = 8.0 nM 8.10
CHEMBL430374 Ki = 21.0 nM 7.68
CHEMBL240279 Ki = 32.0 nM 7.50
CHEMBL391031 Ki = 51.0 nM 7.29
CHEMBL392149 TECADENOSON Ki = 65.0 nM 7.19
CHEMBL391029 Ki = 70.0 nM 7.16
CHEMBL240487 Ki = 164.0 nM 6.79
CHEMBL240278 Ki = 288.0 nM 6.54
CHEMBL392720 Ki = 783.0 nM 6.11
CHEMBL391030 Ki = 803.0 nM 6.09
CHEMBL240277 Ki = 929.0 nM 6.03