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Assay Detail

CHEMBL616210

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

Binding
In vitro binding affinity towards 5-hydroxytryptamine 1A receptor was determined using radioligand [3H]-8-OH-DPAT
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties.
López-Rodríguez ML, Morcillo MJ, Fernández E, Porras E, Orensanz L, Beneytez ME, Manzanares J, Fuentes JA.
J Med Chem (2001) 44 : 186 -197
PubMed 11170628 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.54 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204234 1 8.92
CHEMBL1204241 1 8.44
CHEMBL1204235 1 8.43
CHEMBL1204239 1 8.41
CHEMBL1204250 1 8.40
CHEMBL1204254 1 8.19
CHEMBL1204232 1 8.07
CHEMBL1204230 1 7.96
CHEMBL1204253 1 7.85
CHEMBL1204237 1 7.80
CHEMBL1204236 1 7.62
CHEMBL1204240 1 7.57
CHEMBL1204258 1 7.57
CHEMBL1204203 1 7.57
CHEMBL1204238 1 7.51
CHEMBL1204229 1 7.48
CHEMBL1204244 1 7.48
CHEMBL1204257 1 7.36
CHEMBL1204248 1 7.22
CHEMBL1204231 1 7.10
CHEMBL1202594 1 6.99
CHEMBL1204243 1 6.96
CHEMBL1204246 1 6.90
CHEMBL1204245 1 6.87
CHEMBL1204252 1 6.77
CHEMBL1204255 1 6.67
CHEMBL1204247 1 6.49
CHEMBL1204233 1 6.47
CHEMBL1204228 1 -
CHEMBL1204249 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204234 Ki = 1.2 nM 8.92
CHEMBL1204241 Ki = 3.6 nM 8.44
CHEMBL1204235 Ki = 3.7 nM 8.43
CHEMBL1204239 Ki = 3.9 nM 8.41
CHEMBL1204250 Ki = 4.0 nM 8.40
CHEMBL1204254 Ki = 6.5 nM 8.19
CHEMBL1204232 Ki = 8.6 nM 8.07
CHEMBL1204230 Ki = 11.0 nM 7.96
CHEMBL1204253 Ki = 14.0 nM 7.85
CHEMBL1204237 Ki = 16.0 nM 7.80
CHEMBL1204236 Ki = 24.0 nM 7.62
CHEMBL1204240 Ki = 27.0 nM 7.57
CHEMBL1204258 Ki = 27.0 nM 7.57
CHEMBL1204203 Ki = 27.0 nM 7.57
CHEMBL1204238 Ki = 31.0 nM 7.51
CHEMBL1204244 Ki = 33.0 nM 7.48
CHEMBL1204229 Ki = 33.0 nM 7.48
CHEMBL1204257 Ki = 44.0 nM 7.36
CHEMBL1204248 Ki = 60.0 nM 7.22
CHEMBL1204231 Ki = 80.0 nM 7.10
CHEMBL1202594 Ki = 102.0 nM 6.99
CHEMBL1204243 Ki = 110.0 nM 6.96
CHEMBL1204246 Ki = 126.0 nM 6.90
CHEMBL1204245 Ki = 134.0 nM 6.87
CHEMBL1204252 Ki = 169.0 nM 6.77
CHEMBL1204255 Ki = 214.0 nM 6.67
CHEMBL1204247 Ki = 326.0 nM 6.49
CHEMBL1204233 Ki = 341.0 nM 6.47
CHEMBL1204228 Ki > 1000.0 nM -
CHEMBL1204249 Ki > 1000.0 nM -
CHEMBL1204242 Ki > 1000.0 nM -
CHEMBL1204251 Ki > 1000.0 nM -
CHEMBL1204256 Ki > 10000.0 nM -