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Assay Detail

CHEMBL648030

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

Binding
Binding affinity towards alpha-1 adrenergic receptor using [3H]prazosin radioligand.
ChEMBL ↗
50
Total Activities
50
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 structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist.
López-Rodríguez ML, Rosado ML, Benhamú B, Morcillo MJ, Sanz AM, Orensanz L, Beneitez ME, Fuentes JA, Manzanares J.
J Med Chem (1996) 39 : 4439 -4450
PubMed 8893838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 7.32 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8618 NAN-190 — 1 9.10
CHEMBL289873 — — 1 8.51
CHEMBL42810 — — 1 8.08
CHEMBL46881 — — 1 8.07
CHEMBL290039 — — 1 8.02
CHEMBL43992 — — 1 8.00
CHEMBL296413 — — 1 7.98
CHEMBL41978 — — 1 7.94
CHEMBL42644 — — 1 7.92
CHEMBL290203 — — 1 7.81
CHEMBL44786 — — 1 7.75
CHEMBL42404 — — 1 7.73
CHEMBL416984 — — 1 7.67
CHEMBL46677 — — 1 7.60
CHEMBL45007 — — 1 7.59
CHEMBL43332 — — 1 7.58
CHEMBL46885 — — 1 7.33
CHEMBL46918 — — 1 7.19
CHEMBL417709 — — 1 7.14
CHEMBL45253 — — 1 7.04
CHEMBL42706 — — 1 6.96
CHEMBL296713 — — 1 6.88
CHEMBL297844 — — 1 6.87
CHEMBL46535 — — 1 6.72
CHEMBL47040 — — 1 6.61
CHEMBL297887 — — 1 6.54
CHEMBL49 BUSPIRONE 4.0 1 6.43
CHEMBL46525 — — 1 6.43
CHEMBL46802 — — 1 6.30
CHEMBL46471 — — 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8618 NAN-190 Ki = 0.8 nM 9.10
CHEMBL289873 — Ki = 3.1 nM 8.51
CHEMBL42810 — Ki = 8.3 nM 8.08
CHEMBL46881 — Ki = 8.6 nM 8.07
CHEMBL290039 — Ki = 9.6 nM 8.02
CHEMBL43992 — Ki = 9.9 nM 8.00
CHEMBL296413 — Ki = 10.4 nM 7.98
CHEMBL41978 — Ki = 11.4 nM 7.94
CHEMBL42644 — Ki = 12.1 nM 7.92
CHEMBL290203 — Ki = 15.4 nM 7.81
CHEMBL44786 — Ki = 17.9 nM 7.75
CHEMBL42404 — Ki = 18.6 nM 7.73
CHEMBL416984 — Ki = 21.6 nM 7.67
CHEMBL46677 — Ki = 25.2 nM 7.60
CHEMBL45007 — Ki = 25.8 nM 7.59
CHEMBL43332 — Ki = 26.4 nM 7.58
CHEMBL46885 — Ki = 47.2 nM 7.33
CHEMBL46918 — Ki = 64.9 nM 7.19
CHEMBL417709 — Ki = 72.4 nM 7.14
CHEMBL45253 — Ki = 90.4 nM 7.04
CHEMBL42706 — Ki = 109.0 nM 6.96
CHEMBL296713 — Ki = 131.0 nM 6.88
CHEMBL297844 — Ki = 135.0 nM 6.87
CHEMBL46535 — Ki = 190.0 nM 6.72
CHEMBL47040 — Ki = 247.0 nM 6.61
CHEMBL297887 — Ki = 292.0 nM 6.54
CHEMBL46525 — Ki = 375.0 nM 6.43
CHEMBL49 BUSPIRONE Ki = 367.0 nM 6.43
CHEMBL46802 — Ki = 500.0 nM 6.30
CHEMBL46471 — Ki = 500.0 nM 6.30
CHEMBL46672 — Ki = 869.0 nM 6.06
CHEMBL46470 — Ki = 1000.0 nM 6.00
CHEMBL295527 — Ki > 10000.0 nM -
CHEMBL46862 — Ki > 10000.0 nM -
CHEMBL291165 — Ki > 1000.0 nM -
CHEMBL47200 — Ki > 1000.0 nM -
CHEMBL42219 — Ki > 10000.0 nM -
CHEMBL432495 — Ki > 1000.0 nM -
CHEMBL46651 — Ki > 10000.0 nM -
CHEMBL295244 — Ki > 1000.0 nM -
CHEMBL295168 — Ki > 1000.0 nM -
CHEMBL289784 — Ki > 1000.0 nM -
CHEMBL44876 — Ki > 1000.0 nM -
CHEMBL42654 — Ki > 1000.0 nM -
CHEMBL42396 — Ki > 1000.0 nM -
CHEMBL296724 — Ki > 1000.0 nM -
CHEMBL42881 — Ki > 1000.0 nM -
CHEMBL46377 — Ki > 1000.0 nM -
CHEMBL298286 — Ki > 1000.0 nM -
CHEMBL430567 — Ki > 1000.0 nM -