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Assay Detail

CHEMBL649340

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor via standard competitive displacement assay using rat brain homogenate with [3H]prazosin as radioligand
ChEMBL ↗
68
Total Activities
68
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

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
Zhao H, Thurkauf A, He X, Hodgetts K, Zhang X, Rachwal S, Kover RX, Hutchison A, Peterson J, Kieltyka A, Brodbeck R, Primus R, Wasley JW.
Bioorg Med Chem Lett (2002) 12 : 3105 -3109
PubMed 12372512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 68 6.04 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104380 — — 1 7.44
CHEMBL69584 — — 1 7.06
CHEMBL105011 — — 1 7.02
CHEMBL104273 — — 1 6.99
CHEMBL323022 — — 1 6.94
CHEMBL106742 — — 1 6.93
CHEMBL104719 — — 1 6.93
CHEMBL104832 — — 1 6.90
CHEMBL104579 — — 1 6.85
CHEMBL104800 — — 1 6.79
CHEMBL104788 — — 1 6.79
CHEMBL419356 — — 1 6.63
CHEMBL104432 — — 1 6.58
CHEMBL419916 — — 1 6.50
CHEMBL104716 — — 1 6.49
CHEMBL320440 — — 1 6.30
CHEMBL104138 — — 1 6.29
CHEMBL104399 — — 1 6.23
CHEMBL322326 — — 1 6.22
CHEMBL104614 — — 1 6.17
CHEMBL323525 — — 1 6.06
CHEMBL441274 — — 1 6.04
CHEMBL106751 — — 1 6.03
CHEMBL107962 — — 1 6.01
CHEMBL319650 — — 1 6.01
CHEMBL104498 — — 1 6.00
CHEMBL106598 — — 1 6.00
CHEMBL108157 — — 1 5.98
CHEMBL321538 — — 1 5.93
CHEMBL107742 — — 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104380 — Ki = 36.0 nM 7.44
CHEMBL69584 — Ki = 88.0 nM 7.06
CHEMBL105011 — Ki = 95.0 nM 7.02
CHEMBL104273 — Ki = 103.0 nM 6.99
CHEMBL323022 — Ki = 115.0 nM 6.94
CHEMBL106742 — Ki = 118.0 nM 6.93
CHEMBL104719 — Ki = 118.0 nM 6.93
CHEMBL104832 — Ki = 127.0 nM 6.90
CHEMBL104579 — Ki = 142.0 nM 6.85
CHEMBL104800 — Ki = 161.0 nM 6.79
CHEMBL104788 — Ki = 162.0 nM 6.79
CHEMBL419356 — Ki = 236.0 nM 6.63
CHEMBL104432 — Ki = 261.0 nM 6.58
CHEMBL419916 — Ki = 320.0 nM 6.50
CHEMBL104716 — Ki = 327.0 nM 6.49
CHEMBL320440 — Ki = 504.0 nM 6.30
CHEMBL104138 — Ki = 508.0 nM 6.29
CHEMBL104399 — Ki = 594.0 nM 6.23
CHEMBL322326 — Ki = 598.0 nM 6.22
CHEMBL104614 — Ki = 671.0 nM 6.17
CHEMBL323525 — Ki = 872.0 nM 6.06
CHEMBL441274 — Ki = 909.0 nM 6.04
CHEMBL106751 — Ki = 937.0 nM 6.03
CHEMBL107962 — Ki = 983.0 nM 6.01
CHEMBL319650 — Ki = 972.0 nM 6.01
CHEMBL104498 — Ki = 1000.0 nM 6.00
CHEMBL106598 — Ki = 988.0 nM 6.00
CHEMBL108157 — Ki = 1052.0 nM 5.98
CHEMBL321538 — Ki = 1184.0 nM 5.93
CHEMBL107742 — Ki = 1257.0 nM 5.90
CHEMBL107351 — Ki = 1300.0 nM 5.89
CHEMBL104256 — Ki = 1324.0 nM 5.88
CHEMBL104063 — Ki = 1694.0 nM 5.77
CHEMBL320067 — Ki = 1800.0 nM 5.75
CHEMBL107804 — Ki = 2056.0 nM 5.69
CHEMBL104299 — Ki = 2076.0 nM 5.68
CHEMBL107793 — Ki = 2202.0 nM 5.66
CHEMBL104238 — Ki = 2298.0 nM 5.64
CHEMBL326670 — Ki = 2544.0 nM 5.59
CHEMBL107229 — Ki = 2624.0 nM 5.58
CHEMBL106916 — Ki = 2655.0 nM 5.58
CHEMBL326250 — Ki = 2834.0 nM 5.55
CHEMBL107384 — Ki = 2845.0 nM 5.55
CHEMBL105595 — Ki = 2805.0 nM 5.55
CHEMBL317266 — Ki = 3122.0 nM 5.51
CHEMBL319927 — Ki = 3386.0 nM 5.47
CHEMBL318739 — Ki = 3545.0 nM 5.45
CHEMBL106208 — Ki = 4165.0 nM 5.38
CHEMBL324867 — Ki = 4819.0 nM 5.32
CHEMBL317879 — Ki = 5006.0 nM 5.30