Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL645688

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

Binding
Tested in vitro for binding affinity by measuring its ability to inhibit [3H]prazosin binding at alpha-1 adrenergic receptor in rat cerebral cortex membranes.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
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. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models.
López-Rodríguez ML, Rosado ML, Benhamú B, Morcillo MJ, Fernández E, Schaper KJ.
J Med Chem (1997) 40 : 1648 -1656
PubMed 9171874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.17 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
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
CHEMBL46535 1 6.72
CHEMBL47040 1 6.61
CHEMBL46525 1 6.43
CHEMBL46802 1 6.30
CHEMBL47200 1 5.41
CHEMBL42396 1 5.36
CHEMBL298286 1 5.18
CHEMBL46377 1 5.12
CHEMBL1202594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
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
CHEMBL46535 Ki = 190.0 nM 6.72
CHEMBL47040 Ki = 247.0 nM 6.61
CHEMBL46525 Ki = 375.0 nM 6.43
CHEMBL46802 Ki = 500.0 nM 6.30
CHEMBL47200 Ki = 3935.0 nM 5.41
CHEMBL42396 Ki = 4325.0 nM 5.36
CHEMBL298286 Ki = 6652.0 nM 5.18
CHEMBL46377 Ki = 7533.0 nM 5.12
CHEMBL1202594 Ki > 10000.0 nM -
CHEMBL42219 Ki = 199000.0 nM -
CHEMBL46651 Ki = 260000.0 nM -