Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4670398

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

ADMET
Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat cortex membranes measured after 30 mins by Microbeta2 scintillation counting method
34
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile.
Sniecikowska J,Gluch-Lutwin M,Bucki A,Więckowska A,Siwek A,Jastrzebska-Wiesek M,Partyka A,Wilczyńska D,Pytka K,Latacz G,Przejczowska-Pomierny K,Wyska E,Wesołowska A,Pawłowski M,Newman-Tancredi A,Kolaczkowski M
J Med Chem (2020) 63 : 10946 -10971
PubMed 32883072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.75 7.76
pKi 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790600 1 7.76
CHEMBL4800575 1 7.34
CHEMBL4751777 1 7.18
CHEMBL4756233 1 7.00
CHEMBL4756041 1 6.76
CHEMBL4744067 1 6.72
CHEMBL4756322 1 6.71
CHEMBL4743868 1 6.69
CHEMBL4757755 1 6.36
CHEMBL4741857 1 6.29
CHEMBL4752833 1 6.20
CHEMBL4781985 1 6.04
CHEMBL4797282 1 -
CHEMBL4759759 1 -
CHEMBL4797752 1 -
CHEMBL4786067 1 -
CHEMBL4790662 1 -
CHEMBL4747083 1 -
CHEMBL4753394 1 -
CHEMBL230963 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL4750444 1 -
CHEMBL4777581 1 -
CHEMBL4796345 1 -
CHEMBL4760666 1 -
CHEMBL4755058 1 -
CHEMBL4752177 1 -
CHEMBL4760621 1 -
CHEMBL4740430 1 -
CHEMBL49 BUSPIRONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790600 Ki = 17.38 nM 7.76
CHEMBL4800575 Ki = 45.71 nM 7.34
CHEMBL4751777 Ki = 66.07 nM 7.18
CHEMBL4756233 Ki = 100.0 nM 7.00
CHEMBL4756041 Ki = 173.78 nM 6.76
CHEMBL4744067 Ki = 190.55 nM 6.72
CHEMBL4756322 Ki = 194.98 nM 6.71
CHEMBL4743868 Ki = 204.17 nM 6.69
CHEMBL4757755 Ki = 436.52 nM 6.36
CHEMBL4741857 Ki = 512.86 nM 6.29
CHEMBL4752833 Ki = 630.96 nM 6.20
CHEMBL4781985 Ki = 912.01 nM 6.04
CHEMBL4760271 Ki > 1000.0 nM -
CHEMBL4739908 Ki > 1000.0 nM -
CHEMBL4747425 Ki > 1000.0 nM -
CHEMBL4746386 Ki > 1000.0 nM -
CHEMBL4797282 Ki > 1000.0 nM -
CHEMBL4759759 Ki > 1000.0 nM -
CHEMBL4797752 Ki > 1000.0 nM -
CHEMBL4786067 Ki > 1000.0 nM -
CHEMBL4790662 Ki > 1000.0 nM -
CHEMBL4747083 Ki > 1000.0 nM -
CHEMBL4753394 Ki > 1000.0 nM -
CHEMBL230963 Ki > 1000.0 nM -
CHEMBL56 8-OH-DPAT pKi - -
CHEMBL4750444 Ki > 1000.0 nM -
CHEMBL4777581 Ki > 1000.0 nM -
CHEMBL4796345 Ki > 1000.0 nM -
CHEMBL4760666 Ki > 1000.0 nM -
CHEMBL4755058 Ki > 1000.0 nM -
CHEMBL4752177 Ki > 1000.0 nM -
CHEMBL4760621 Ki > 1000.0 nM -
CHEMBL4740430 Ki > 1000.0 nM -
CHEMBL49 BUSPIRONE pKi - -