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Assay Detail

CHEMBL643449

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

Binding
Inhibition of [3H]WB-4101 binding to rat cortical Alpha-1 adrenergic receptor in vitro
23
Total Activities
23
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

Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
Yevich JP, New JS, Lobeck WG, Dextraze P, Bernstein E, Taylor DP, Yocca FD, Eison MS, Temple DL.
J Med Chem (1992) 35 : 4516 -4525
PubMed 1361578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.70 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140872 1 8.22
CHEMBL141226 1 7.66
CHEMBL140656 1 7.54
CHEMBL137870 1 7.29
CHEMBL479 THIORIDAZINE 4.0 1 7.19
CHEMBL141922 1 7.14
CHEMBL141455 1 7.02
CHEMBL335348 1 6.79
CHEMBL141854 1 6.75
CHEMBL334934 1 6.64
CHEMBL443482 1 6.58
CHEMBL140650 1 6.52
CHEMBL342484 1 6.43
CHEMBL140831 1 6.40
CHEMBL137967 1 6.35
CHEMBL60859 BMY-14802 1 6.28
CHEMBL344577 1 6.12
CHEMBL140712 1 6.09
CHEMBL138186 1 5.94
CHEMBL139595 1 5.85
CHEMBL141670 1 5.82
CHEMBL140833 1 -
CHEMBL141523 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140872 IC50 = 6.0 nM 8.22
CHEMBL141226 IC50 = 22.0 nM 7.66
CHEMBL140656 IC50 = 29.0 nM 7.54
CHEMBL137870 IC50 = 51.0 nM 7.29
CHEMBL479 THIORIDAZINE IC50 = 65.0 nM 7.19
CHEMBL141922 IC50 = 72.0 nM 7.14
CHEMBL141455 IC50 = 95.0 nM 7.02
CHEMBL335348 IC50 = 162.0 nM 6.79
CHEMBL141854 IC50 = 180.0 nM 6.75
CHEMBL334934 IC50 = 230.0 nM 6.64
CHEMBL443482 IC50 = 266.0 nM 6.58
CHEMBL140650 IC50 = 305.0 nM 6.52
CHEMBL342484 IC50 = 375.0 nM 6.43
CHEMBL140831 IC50 = 400.0 nM 6.40
CHEMBL137967 IC50 = 446.0 nM 6.35
CHEMBL60859 BMY-14802 IC50 = 520.0 nM 6.28
CHEMBL344577 IC50 = 756.0 nM 6.12
CHEMBL140712 IC50 = 814.0 nM 6.09
CHEMBL138186 IC50 = 1140.0 nM 5.94
CHEMBL139595 IC50 = 1420.0 nM 5.85
CHEMBL141670 IC50 = 1500.0 nM 5.82
CHEMBL140833 IC50 > 1000.0 nM -
CHEMBL141523 IC50 > 1000.0 nM -