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Assay Detail

CHEMBL642091

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

Binding
Binding affinity at Alpha-1 adrenergic receptor by inhibition of [3H]-prazosin binding to rat cortex
27
Total Activities
27
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

Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
Peglion JL, Goument B, Despaux N, Charlot V, Giraud H, Nisole C, Newman-Tancredi A, Dekeyne A, Bertrand M, Genissel P, Millan MJ.
J Med Chem (2002) 45 : 165 -176
PubMed 11754589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.82 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51882 1 7.77
CHEMBL45966 1 7.64
CHEMBL48767 1 7.53
CHEMBL301806 1 7.44
CHEMBL48713 1 7.34
CHEMBL297017 1 7.26
CHEMBL298855 1 7.22
CHEMBL51457 1 7.19
CHEMBL47433 1 7.10
CHEMBL50119 1 7.10
CHEMBL48876 1 7.08
CHEMBL49497 1 7.00
CHEMBL300739 1 6.96
CHEMBL410530 1 6.95
CHEMBL49247 1 6.90
CHEMBL49838 1 6.90
CHEMBL299817 1 6.67
CHEMBL298096 1 6.57
CHEMBL298279 1 6.55
CHEMBL300879 1 6.31
CHEMBL412357 1 6.17
CHEMBL300100 1 6.15
CHEMBL50903 1 6.15
CHEMBL49206 1 6.13
CHEMBL297925 1 6.07
CHEMBL298363 1 6.03
CHEMBL299405 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51882 Ki = 16.98 nM 7.77
CHEMBL45966 Ki = 22.91 nM 7.64
CHEMBL48767 Ki = 29.51 nM 7.53
CHEMBL301806 Ki = 36.31 nM 7.44
CHEMBL48713 Ki = 45.71 nM 7.34
CHEMBL297017 Ki = 54.95 nM 7.26
CHEMBL298855 Ki = 60.26 nM 7.22
CHEMBL51457 Ki = 64.57 nM 7.19
CHEMBL47433 Ki = 79.43 nM 7.10
CHEMBL50119 Ki = 79.43 nM 7.10
CHEMBL48876 Ki = 83.18 nM 7.08
CHEMBL49497 Ki = 100.0 nM 7.00
CHEMBL300739 Ki = 109.65 nM 6.96
CHEMBL410530 Ki = 112.2 nM 6.95
CHEMBL49247 Ki = 125.89 nM 6.90
CHEMBL49838 Ki = 125.89 nM 6.90
CHEMBL299817 Ki = 213.8 nM 6.67
CHEMBL298096 Ki = 269.15 nM 6.57
CHEMBL298279 Ki = 281.84 nM 6.55
CHEMBL300879 Ki = 489.78 nM 6.31
CHEMBL412357 Ki = 676.08 nM 6.17
CHEMBL300100 Ki = 707.95 nM 6.15
CHEMBL50903 Ki = 707.95 nM 6.15
CHEMBL49206 Ki = 741.31 nM 6.13
CHEMBL297925 Ki = 851.14 nM 6.07
CHEMBL298363 Ki = 933.25 nM 6.03
CHEMBL299405 Ki = 933.25 nM 6.03