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Assay Detail

CHEMBL982305

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

Binding
Displacement of [3H]prazosin from alpha1 adrenergic receptor in Wistar rat cerebral cortex membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action.
Iturriaga-Vásquez P, Miquel R, Ivorra MD, D'Ocon MP, Cassels BK.
J Nat Prod (2003) 66 : 954 -957
PubMed 12880313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.37 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176045 FANCHININ 1 6.16
CHEMBL453291 COCLAURINE 1 5.97
CHEMBL509109 1 5.73
CHEMBL451988 1 5.69
CHEMBL453292 METHYL COCLAURINE 1 5.63
CHEMBL510364 1 5.49
CHEMBL455620 1 5.49
CHEMBL507843 1 5.34
CHEMBL453293 1 5.29
CHEMBL451987 1 5.29
CHEMBL510363 1 5.23
CHEMBL451722 1 5.14
CHEMBL452763 1 5.12
CHEMBL452500 1 5.10
CHEMBL114853 1 5.07
CHEMBL453024 1 5.05
CHEMBL452762 1 5.02
CHEMBL451723 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176045 FANCHININ Ki = 691.83 nM 6.16
CHEMBL453291 COCLAURINE Ki = 1071.52 nM 5.97
CHEMBL509109 Ki = 1862.09 nM 5.73
CHEMBL451988 Ki = 2041.74 nM 5.69
CHEMBL453292 METHYL COCLAURINE Ki = 2344.23 nM 5.63
CHEMBL510364 Ki = 3235.94 nM 5.49
CHEMBL455620 Ki = 3235.94 nM 5.49
CHEMBL507843 Ki = 4570.88 nM 5.34
CHEMBL453293 Ki = 5128.61 nM 5.29
CHEMBL451987 Ki = 5128.61 nM 5.29
CHEMBL510363 Ki = 5888.44 nM 5.23
CHEMBL451722 Ki = 7244.36 nM 5.14
CHEMBL452763 Ki = 7585.78 nM 5.12
CHEMBL452500 Ki = 7943.28 nM 5.10
CHEMBL114853 Ki = 8511.38 nM 5.07
CHEMBL453024 Ki = 8912.51 nM 5.05
CHEMBL452762 Ki = 9549.93 nM 5.02
CHEMBL451723 Ki = 12022.64 nM 4.92