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Assay Detail

CHEMBL650229

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

Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Bishop MJ, Barvian KA, Berman J, Bigham EC, Garrison DT, Gobel MJ, Hodson SJ, Irving PE, Liacos JA, Navas F, Saussy DL, Speake JD.
Bioorg Med Chem Lett (2002) 12 : 471 -475
PubMed 11814822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 8.01 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL422477 1 9.60
CHEMBL142784 1 9.30
CHEMBL143801 1 9.00
CHEMBL279136 1 8.90
CHEMBL357129 1 8.90
CHEMBL356605 1 8.70
CHEMBL143973 1 8.60
CHEMBL142871 1 8.60
CHEMBL13789 1 8.50
CHEMBL143562 1 8.50
CHEMBL142387 1 8.30
CHEMBL344551 1 8.30
CHEMBL337862 1 8.10
CHEMBL341747 1 7.90
CHEMBL13852 CIRAZOLINE 2.0 1 7.90
CHEMBL420683 1 7.90
CHEMBL344957 1 7.60
CHEMBL142958 1 7.60
CHEMBL421011 1 7.50
CHEMBL142967 1 7.40
CHEMBL142864 1 7.00
CHEMBL342324 1 6.90
CHEMBL143766 1 6.80
CHEMBL72958 NS-49 1 6.50
CHEMBL358802 1 5.90
CHEMBL344294 1 -
CHEMBL144956 1 -
CHEMBL142310 1 -
CHEMBL141986 1 -
CHEMBL117914 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL422477 EC50 = 0.2512 nM 9.60
CHEMBL142784 EC50 = 0.5012 nM 9.30
CHEMBL143801 EC50 = 1.0 nM 9.00
CHEMBL279136 EC50 = 1.259 nM 8.90
CHEMBL357129 EC50 = 1.259 nM 8.90
CHEMBL356605 EC50 = 1.995 nM 8.70
CHEMBL143973 EC50 = 2.512 nM 8.60
CHEMBL142871 EC50 = 2.512 nM 8.60
CHEMBL13789 EC50 = 3.162 nM 8.50
CHEMBL143562 EC50 = 3.162 nM 8.50
CHEMBL142387 EC50 = 5.012 nM 8.30
CHEMBL344551 EC50 = 5.012 nM 8.30
CHEMBL337862 EC50 = 7.943 nM 8.10
CHEMBL341747 EC50 = 12.59 nM 7.90
CHEMBL13852 CIRAZOLINE EC50 = 12.59 nM 7.90
CHEMBL420683 EC50 = 12.59 nM 7.90
CHEMBL344957 EC50 = 25.12 nM 7.60
CHEMBL142958 EC50 = 25.12 nM 7.60
CHEMBL421011 EC50 = 31.62 nM 7.50
CHEMBL142967 EC50 = 39.81 nM 7.40
CHEMBL142864 EC50 = 100.0 nM 7.00
CHEMBL342324 EC50 = 125.89 nM 6.90
CHEMBL143766 EC50 = 158.49 nM 6.80
CHEMBL72958 NS-49 EC50 = 316.23 nM 6.50
CHEMBL358802 EC50 = 1258.93 nM 5.90
CHEMBL344294 EC50 < 100000.0 nM -
CHEMBL144956 EC50 < 100000.0 nM -
CHEMBL142310 EC50 < 100000.0 nM -
CHEMBL141986 EC50 < 100000.0 nM -
CHEMBL117914 EC50 < 5011.87 nM -