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Assay Detail

CHEMBL645215

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

Binding
Ex vivo inhibition of guinea pig ileum twitch via Adenosine A1 receptor.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL2304404)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

The discovery and synthesis of highly potent, A2a receptor agonists.
Keeling SE, Albinson FD, Ayres BE, Butchers PR, Chambers CL, Cherry PC, Ellis F, Ewan GB, Gregson M, Knight J, Mills K, Ravenscroft P, Reynolds LH, Sanjar S, Sheehan MJ.
Bioorg Med Chem Lett (2000) 10 : 403 -406
PubMed 10714510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.10 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 9.00
CHEMBL284969 1 9.00
CHEMBL131280 1 8.70
CHEMBL340674 1 7.10
CHEMBL131535 1 7.08
CHEMBL131242 1 6.58
CHEMBL130830 1 6.58
CHEMBL337080 1 6.43
CHEMBL131457 1 6.41
CHEMBL128176 1 6.26
CHEMBL336608 1 6.17
CHEMBL334336 1 5.83
CHEMBL435188 1 -
CHEMBL339522 1 -
CHEMBL131175 1 -
CHEMBL341031 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 1.0 nM 9.00
CHEMBL284969 Ki = 1.0 nM 9.00
CHEMBL131280 Ki = 2.0 nM 8.70
CHEMBL340674 Ki = 80.0 nM 7.10
CHEMBL131535 Ki = 84.0 nM 7.08
CHEMBL131242 Ki = 263.0 nM 6.58
CHEMBL130830 Ki = 260.0 nM 6.58
CHEMBL337080 Ki = 369.0 nM 6.43
CHEMBL131457 Ki = 390.0 nM 6.41
CHEMBL128176 Ki = 549.0 nM 6.26
CHEMBL336608 Ki = 672.0 nM 6.17
CHEMBL334336 Ki = 1470.0 nM 5.83
CHEMBL435188 Ki > 5000.0 nM -
CHEMBL339522 Ki > 1000.0 nM -
CHEMBL131175 Ki > 612.0 nM -
CHEMBL341031 Ki - nM -