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Assay Detail

CHEMBL642096

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor using prazosin as a radioligand in rat cortex
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C, Kleven M.
J Med Chem (1999) 42 : 1648 -1660
PubMed 10229633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.59 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44118 1 6.92
CHEMBL42994 1 6.92
CHEMBL44904 1 6.87
CHEMBL295662 1 6.86
CHEMBL42766 1 6.81
CHEMBL42618 1 6.76
CHEMBL46971 1 6.76
CHEMBL46467 1 6.75
CHEMBL288244 1 6.72
CHEMBL42294 1 6.71
CHEMBL360319 1 6.68
CHEMBL45101 1 6.66
CHEMBL298260 1 6.64
CHEMBL297138 1 6.55
CHEMBL43146 1 6.39
CHEMBL45423 1 6.35
CHEMBL46512 1 6.26
CHEMBL42393 1 6.12
CHEMBL46582 1 6.10
CHEMBL44659 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44118 Ki = 120.23 nM 6.92
CHEMBL42994 Ki = 120.23 nM 6.92
CHEMBL44904 Ki = 134.9 nM 6.87
CHEMBL295662 Ki = 138.04 nM 6.86
CHEMBL42766 Ki = 154.88 nM 6.81
CHEMBL42618 Ki = 173.78 nM 6.76
CHEMBL46971 Ki = 173.78 nM 6.76
CHEMBL46467 Ki = 177.83 nM 6.75
CHEMBL288244 Ki = 190.55 nM 6.72
CHEMBL42294 Ki = 194.98 nM 6.71
CHEMBL360319 Ki = 208.93 nM 6.68
CHEMBL45101 Ki = 218.78 nM 6.66
CHEMBL298260 Ki = 229.09 nM 6.64
CHEMBL297138 Ki = 281.84 nM 6.55
CHEMBL43146 Ki = 407.38 nM 6.39
CHEMBL45423 Ki = 446.68 nM 6.35
CHEMBL46512 Ki = 549.54 nM 6.26
CHEMBL42393 Ki = 758.58 nM 6.12
CHEMBL46582 Ki = 794.33 nM 6.10
CHEMBL44659 Ki = 1258.93 nM 5.90