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Assay Detail

CHEMBL642097

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

Binding
Binding affinity determined to alpha-1 adrenergic receptor of rat cerebral cortex using [3H]prazosin as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site.
Clark RD, Berger J, Garg P, Weinhardt KK, Spedding M, Kilpatrick AT, Brown CM, MacKinnon AC.
J Med Chem (1990) 33 : 596 -600
PubMed 2153820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.50 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15245 YOHIMBINE 3.0 1 6.40
CHEMBL10316 IDAZOXAN 3.0 1 6.10
CHEMBL2448022 1 6.05
CHEMBL2448029 1 5.80
CHEMBL2448027 1 5.68
CHEMBL1203553 1 5.67
CHEMBL1203556 1 5.55
CHEMBL1203560 1 5.50
CHEMBL2448025 1 5.50
CHEMBL1203563 1 5.43
CHEMBL1203561 1 5.26
CHEMBL2448026 1 5.20
CHEMBL1203566 1 5.19
CHEMBL1203554 1 5.14
CHEMBL1203571 1 4.80
CHEMBL1203559 1 4.72
CHEMBL1203569 1 -
CHEMBL1203552 1 -
CHEMBL1203570 1 -
CHEMBL1203558 1 -
CHEMBL1203562 1 -
CHEMBL1203557 1 -
CHEMBL2448023 1 -
CHEMBL2448028 1 -
CHEMBL1203555 1 -
CHEMBL2448024 1 -
CHEMBL1203565 1 -
CHEMBL1203564 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15245 YOHIMBINE Ki = 398.11 nM 6.40
CHEMBL10316 IDAZOXAN Ki = 794.33 nM 6.10
CHEMBL2448022 Ki = 891.25 nM 6.05
CHEMBL2448029 Ki = 1584.89 nM 5.80
CHEMBL2448027 Ki = 2089.3 nM 5.68
CHEMBL1203553 Ki = 2137.96 nM 5.67
CHEMBL1203556 Ki = 2818.38 nM 5.55
CHEMBL1203560 Ki = 3162.28 nM 5.50
CHEMBL2448025 Ki = 3162.28 nM 5.50
CHEMBL1203563 Ki = 3715.35 nM 5.43
CHEMBL1203561 Ki = 5495.41 nM 5.26
CHEMBL2448026 Ki = 6309.57 nM 5.20
CHEMBL1203566 Ki = 6456.54 nM 5.19
CHEMBL1203554 Ki = 7244.36 nM 5.14
CHEMBL1203571 Ki = 15848.93 nM 4.80
CHEMBL1203559 Ki = 19054.61 nM 4.72
CHEMBL1203569 Ki < 10000.0 nM -
CHEMBL1203552 Ki < 10000.0 nM -
CHEMBL1203570 Ki < 10000.0 nM -
CHEMBL1203558 Ki < 10000.0 nM -
CHEMBL1203562 Ki < 10000.0 nM -
CHEMBL1203557 Ki < 10000.0 nM -
CHEMBL2448023 Ki < 10000.0 nM -
CHEMBL2448028 Ki < 10000.0 nM -
CHEMBL1203555 Ki < 10000.0 nM -
CHEMBL2448024 Ki < 10000.0 nM -
CHEMBL1203565 Ki < 10000.0 nM -
CHEMBL1203564 Ki < 10000.0 nM -