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Assay Detail

CHEMBL650231

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

Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
31
Total Activities
31
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

2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Navas F, Bishop MJ, Garrison DT, Hodson SJ, Speake JD, Bigham EC, Drewry DH, Saussy DL, Liacos JH, Irving PE, Gobel MJ.
Bioorg Med Chem Lett (2002) 12 : 575 -579
PubMed 11844675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 7.78 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152155 1 9.33
CHEMBL155326 1 9.18
CHEMBL414185 1 9.10
CHEMBL155327 1 9.10
CHEMBL152693 1 9.07
CHEMBL346380 1 8.65
CHEMBL152725 1 8.57
CHEMBL156950 1 8.48
CHEMBL434074 1 8.35
CHEMBL349082 1 8.34
CHEMBL154298 1 8.17
CHEMBL156661 1 8.00
CHEMBL13852 CIRAZOLINE 2.0 1 7.90
CHEMBL154023 1 7.82
CHEMBL117381 1 7.76
CHEMBL762 OXYMETAZOLINE 4.0 1 7.70
CHEMBL356195 1 7.68
CHEMBL154170 1 7.61
CHEMBL351543 1 7.44
CHEMBL347268 1 7.41
CHEMBL156893 1 7.37
CHEMBL154346 1 7.34
CHEMBL351542 1 7.29
CHEMBL346465 1 7.28
CHEMBL761 NAPHAZOLINE 4.0 1 7.20
CHEMBL439822 1 7.06
CHEMBL352225 1 6.96
CHEMBL152154 1 6.49
CHEMBL347920 1 6.18
CHEMBL350906 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152155 EC50 = 0.4677 nM 9.33
CHEMBL155326 EC50 = 0.6607 nM 9.18
CHEMBL414185 EC50 = 0.7943 nM 9.10
CHEMBL155327 EC50 = 0.7943 nM 9.10
CHEMBL152693 EC50 = 0.8511 nM 9.07
CHEMBL346380 EC50 = 2.239 nM 8.65
CHEMBL152725 EC50 = 2.692 nM 8.57
CHEMBL156950 EC50 = 3.311 nM 8.48
CHEMBL434074 EC50 = 4.467 nM 8.35
CHEMBL349082 EC50 = 4.571 nM 8.34
CHEMBL154298 EC50 = 6.761 nM 8.17
CHEMBL156661 EC50 = 10.0 nM 8.00
CHEMBL13852 CIRAZOLINE EC50 = 12.59 nM 7.90
CHEMBL154023 EC50 = 15.14 nM 7.82
CHEMBL117381 EC50 = 17.38 nM 7.76
CHEMBL762 OXYMETAZOLINE EC50 = 19.95 nM 7.70
CHEMBL356195 EC50 = 20.89 nM 7.68
CHEMBL154170 EC50 = 24.55 nM 7.61
CHEMBL351543 EC50 = 36.31 nM 7.44
CHEMBL347268 EC50 = 38.9 nM 7.41
CHEMBL156893 EC50 = 42.66 nM 7.37
CHEMBL154346 EC50 = 45.71 nM 7.34
CHEMBL351542 EC50 = 51.29 nM 7.29
CHEMBL346465 EC50 = 52.48 nM 7.28
CHEMBL761 NAPHAZOLINE EC50 = 63.1 nM 7.20
CHEMBL439822 EC50 = 87.1 nM 7.06
CHEMBL352225 EC50 = 109.65 nM 6.96
CHEMBL152154 EC50 = 323.59 nM 6.49
CHEMBL347920 EC50 = 660.69 nM 6.18
CHEMBL350906 EC50 = 676.08 nM 6.17
CHEMBL358685 EC50 = 724.44 nM 6.14