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Assay Detail

CHEMBL615781

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

Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1 receptor by displacing [3H]5-HT radioligand in rat cerebral cortex
31
Total Activities
31
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

Serotonin 1 (5-HT1) receptor (CHEMBL2095159)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Pyrrole mannich bases as potential antipsychotic agents.
Scott MK, Martin GE, DiStefano DL, Fedde CL, Kukla MJ, Barrett DL, Baldy WJ, Elgin RJ, Kesslick JM, Mathiasen JR.
J Med Chem (1992) 35 : 552 -558
PubMed 1346653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.99 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346168 1 7.74
CHEMBL347334 1 7.56
CHEMBL9666 1 7.55
CHEMBL153136 1 7.53
CHEMBL434512 1 7.48
CHEMBL347056 1 7.39
CHEMBL155506 1 7.38
CHEMBL347782 1 7.30
CHEMBL428175 RWJ-25730 1 7.24
CHEMBL348002 1 7.23
CHEMBL152311 1 7.16
CHEMBL357286 1 7.12
CHEMBL348241 1 7.12
CHEMBL152458 1 7.09
CHEMBL152363 1 6.92
CHEMBL345506 1 6.92
CHEMBL152776 1 6.86
CHEMBL152204 1 6.85
CHEMBL152336 1 6.83
CHEMBL153219 1 6.81
CHEMBL153490 1 6.73
CHEMBL357532 1 6.71
CHEMBL348014 1 6.55
CHEMBL153335 1 6.52
CHEMBL267777 RITANSERIN 2.0 1 6.08
CHEMBL346881 1 6.00
CHEMBL151966 1 6.00
CHEMBL153263 1 -
CHEMBL422 TRIFLUOPERAZINE 4.0 1 -
CHEMBL153161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346168 Ki = 18.1 nM 7.74
CHEMBL347334 Ki = 27.3 nM 7.56
CHEMBL9666 Ki = 28.0 nM 7.55
CHEMBL153136 Ki = 29.3 nM 7.53
CHEMBL434512 Ki = 33.1 nM 7.48
CHEMBL347056 Ki = 41.0 nM 7.39
CHEMBL155506 Ki = 41.3 nM 7.38
CHEMBL347782 Ki = 50.2 nM 7.30
CHEMBL428175 RWJ-25730 Ki = 57.0 nM 7.24
CHEMBL348002 Ki = 58.9 nM 7.23
CHEMBL152311 Ki = 68.8 nM 7.16
CHEMBL357286 Ki = 76.0 nM 7.12
CHEMBL348241 Ki = 76.0 nM 7.12
CHEMBL152458 Ki = 82.1 nM 7.09
CHEMBL152363 Ki = 120.0 nM 6.92
CHEMBL345506 Ki = 120.0 nM 6.92
CHEMBL152776 Ki = 139.0 nM 6.86
CHEMBL152204 Ki = 140.0 nM 6.85
CHEMBL152336 Ki = 148.0 nM 6.83
CHEMBL153219 Ki = 156.0 nM 6.81
CHEMBL153490 Ki = 185.0 nM 6.73
CHEMBL357532 Ki = 196.0 nM 6.71
CHEMBL348014 Ki = 283.0 nM 6.55
CHEMBL153335 Ki = 304.0 nM 6.52
CHEMBL267777 RITANSERIN Ki = 842.0 nM 6.08
CHEMBL346881 Ki = 1000.0 nM 6.00
CHEMBL151966 Ki = 1000.0 nM 6.00
CHEMBL153263 Ki > 1000.0 nM -
CHEMBL422 TRIFLUOPERAZINE Ki > 1000.0 nM -
CHEMBL153161 Ki > 1000.0 nM -
CHEMBL267044 LEVOSULPIRIDE Ki > 1000.0 nM -