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Assay Detail

CHEMBL641400

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

Functional
Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Hodson SJ, Bigham EC, Garrison DT, Gobel MJ, Irving PE, Liacos JA, Navas F, Saussy DL, Sherman BW, Speake JD, Bishop MJ.
Bioorg Med Chem Lett (2002) 12 : 3449 -3452
PubMed 12419381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 7.30 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117248 1 8.10
CHEMBL118055 1 7.70
CHEMBL114669 1 7.50
CHEMBL325745 1 7.10
CHEMBL327005 1 7.00
CHEMBL13852 CIRAZOLINE 2.0 1 6.90
CHEMBL318544 1 6.80
CHEMBL117581 1 -
CHEMBL116843 1 -
CHEMBL115977 1 -
CHEMBL116700 1 -
CHEMBL117094 1 -
CHEMBL117482 1 -
CHEMBL117914 1 -
CHEMBL326837 1 -
CHEMBL13789 1 -
CHEMBL420683 1 -
CHEMBL326067 1 -
CHEMBL117381 1 -
CHEMBL71001 1 -
CHEMBL421011 1 -
CHEMBL325648 1 -
CHEMBL114054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117248 EC50 = 7.943 nM 8.10
CHEMBL118055 EC50 = 19.95 nM 7.70
CHEMBL114669 EC50 = 31.62 nM 7.50
CHEMBL325745 EC50 = 79.43 nM 7.10
CHEMBL327005 EC50 = 100.0 nM 7.00
CHEMBL13852 CIRAZOLINE EC50 = 125.89 nM 6.90
CHEMBL318544 EC50 = 158.49 nM 6.80
CHEMBL117581 EC50 < 5011.87 nM -
CHEMBL116843 EC50 < 100000.0 nM -
CHEMBL115977 EC50 < 100000.0 nM -
CHEMBL116700 EC50 < 100000.0 nM -
CHEMBL117094 EC50 < 100000.0 nM -
CHEMBL117482 EC50 < 5011.87 nM -
CHEMBL117914 EC50 < 100000.0 nM -
CHEMBL326837 EC50 < 100000.0 nM -
CHEMBL13789 EC50 < 100000.0 nM -
CHEMBL420683 EC50 < 100000.0 nM -
CHEMBL326067 EC50 < 251.19 nM -
CHEMBL117381 EC50 < 5011.87 nM -
CHEMBL71001 EC50 < 100000.0 nM -
CHEMBL421011 EC50 < 5011.87 nM -
CHEMBL325648 EC50 < 5011.87 nM -
CHEMBL114054 EC50 < 5011.87 nM -