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Assay Detail

CHEMBL4707368

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

Binding
Displacement of [3H]-prazosin from alpha1 adrenergic receptor in rat cortex measured after 30 mins by microbeta2 scintillation counting method
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel Aryloxyethyl Derivatives of 1-(1-Benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) Phosphorylation-Preferring Serotonin 5-HT Receptor-Biased Agonists with Robust Antidepressant-like Activity.
Sniecikowska J,Gluch-Lutwin M,Bucki A,Więckowska A,Siwek A,Jastrzebska-Wiesek M,Partyka A,Wilczyńska D,Pytka K,Pociecha K,Cios A,Wyska E,Wesołowska A,Pawłowski M,Varney MA,Newman-Tancredi A,Kolaczkowski M
J Med Chem (2019) 62 : 2750 -2771
PubMed 30721053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.93 7.63
pKi 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4759629 1 7.63
CHEMBL4740097 1 7.26
CHEMBL4754941 1 6.89
CHEMBL4753328 1 6.78
CHEMBL4786537 1 6.75
CHEMBL4741857 1 6.29
CHEMBL4789505 1 -
CHEMBL4793515 1 -
CHEMBL4742112 1 -
CHEMBL230963 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL49 BUSPIRONE 4.0 1 -
CHEMBL4742122 1 -
CHEMBL4761382 1 -
CHEMBL4753414 1 -
CHEMBL4745099 1 -
CHEMBL4777084 1 -
CHEMBL4753988 1 -
CHEMBL4748858 1 -
CHEMBL4754363 1 -
CHEMBL4746734 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4759629 Ki = 23.44 nM 7.63
CHEMBL4740097 Ki = 54.95 nM 7.26
CHEMBL4754941 Ki = 128.82 nM 6.89
CHEMBL4753328 Ki = 165.96 nM 6.78
CHEMBL4786537 Ki = 177.83 nM 6.75
CHEMBL4741857 Ki = 512.86 nM 6.29
CHEMBL4789505 Ki > 1000.0 nM -
CHEMBL4793515 pKi - -
CHEMBL4742112 pKi - -
CHEMBL230963 Ki > 1000.0 nM -
CHEMBL56 8-OH-DPAT pKi - -
CHEMBL49 BUSPIRONE pKi - -
CHEMBL4742122 Ki > 1000.0 nM -
CHEMBL4761382 Ki > 1000.0 nM -
CHEMBL4753414 Ki > 1000.0 nM -
CHEMBL4745099 Ki > 1000.0 nM -
CHEMBL4777084 Ki > 1000.0 nM -
CHEMBL4753988 Ki > 1000.0 nM -
CHEMBL4748858 Ki > 1000.0 nM -
CHEMBL4754363 Ki > 1000.0 nM -
CHEMBL4746734 Ki > 1000.0 nM -