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Assay Detail

CHEMBL857994

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

Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor in rat cortex was determined using [3H]prazosin as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
Peglion JL, Canton H, Bervoets K, Audinot V, Brocco M, Gobert A, Le Marouille-Girardon S, Millan MJ.
J Med Chem (1995) 38 : 4044 -4055
PubMed 7562940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.33 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8618 NAN-190 1 9.09
CHEMBL133188 1 7.81
CHEMBL131011 1 7.75
CHEMBL130276 1 7.66
CHEMBL131900 1 7.56
CHEMBL341390 1 7.19
CHEMBL49247 1 6.84
CHEMBL13647 BMY-7378 1 6.74
CHEMBL127216 1 6.68
CHEMBL38288 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8618 NAN-190 Ki = 0.8128 nM 9.09
CHEMBL133188 Ki = 15.49 nM 7.81
CHEMBL131011 Ki = 17.78 nM 7.75
CHEMBL130276 Ki = 21.88 nM 7.66
CHEMBL131900 Ki = 27.54 nM 7.56
CHEMBL341390 Ki = 64.57 nM 7.19
CHEMBL49247 Ki = 144.54 nM 6.84
CHEMBL13647 BMY-7378 Ki = 181.97 nM 6.74
CHEMBL127216 Ki = 208.93 nM 6.68
CHEMBL38288 Ki = 1148.15 nM 5.94