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Assay Detail

CHEMBL645557

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

Binding
Compound was evaluated for inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in rat forebrain homogenate.
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

(alpha S)-erythro-alpha-methylepinephrine: preparation and stereoselective binding to adrenergic receptors in rat forebrain.
Taylor CA, Smith HE, Goldberg MR, Robertson D.
J Med Chem (1981) 24 : 1261 -1263
PubMed 7328589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.52 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL679 EPINEPHRINE 4.0 1 6.70
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.30
CHEMBL677 LEVONORDEFRIN 4.0 3 5.44
CHEMBL2114304 1 4.96
CHEMBL416557 DIOXIFEDRINE 2.0 1 4.55
CHEMBL23040 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL679 EPINEPHRINE Ki = 200.0 nM 6.70
CHEMBL1437 NOREPINEPHRINE Ki = 500.0 nM 6.30
CHEMBL677 LEVONORDEFRIN Ki = 3600.0 nM 5.44
CHEMBL677 LEVONORDEFRIN Ki = 7300.0 nM 5.14
CHEMBL2114304 Ki = 11000.0 nM 4.96
CHEMBL416557 DIOXIFEDRINE Ki = 28000.0 nM 4.55
CHEMBL677 LEVONORDEFRIN Ki = 2315000.0 nM -
CHEMBL23040 Ki = 146000.0 nM -