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Assay Detail

CHEMBL617686

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 2 receptor by displacing [3H]ketanserin radioligand in rat cerebral cortex
30
Total Activities
30
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 2 (5-HT2) receptor (CHEMBL2093870)
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 30 6.66 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267777 RITANSERIN 2.0 1 9.59
CHEMBL422 TRIFLUOPERAZINE 4.0 1 8.28
CHEMBL434512 1 7.26
CHEMBL152458 1 6.96
CHEMBL155506 1 6.86
CHEMBL49 BUSPIRONE 4.0 1 6.76
CHEMBL347782 1 6.71
CHEMBL153335 1 6.64
CHEMBL348002 1 6.62
CHEMBL357532 1 6.59
CHEMBL346168 1 6.58
CHEMBL153136 1 6.57
CHEMBL348014 1 6.50
CHEMBL347334 1 6.45
CHEMBL345506 1 6.41
CHEMBL357286 1 6.39
CHEMBL348241 1 6.34
CHEMBL152363 1 6.17
CHEMBL424332 1 6.17
CHEMBL347056 1 6.00
CHEMBL152311 1 6.00
CHEMBL428175 RWJ-25730 1 6.00
CHEMBL153219 1 6.00
CHEMBL152336 1 6.00
CHEMBL346459 1 -
CHEMBL346881 1 -
CHEMBL153490 1 -
CHEMBL153263 1 -
CHEMBL9666 1 -
CHEMBL267044 LEVOSULPIRIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267777 RITANSERIN Ki = 0.26 nM 9.59
CHEMBL422 TRIFLUOPERAZINE Ki = 5.2 nM 8.28
CHEMBL434512 Ki = 55.3 nM 7.26
CHEMBL152458 Ki = 110.0 nM 6.96
CHEMBL155506 Ki = 137.0 nM 6.86
CHEMBL49 BUSPIRONE Ki = 174.0 nM 6.76
CHEMBL347782 Ki = 196.0 nM 6.71
CHEMBL153335 Ki = 227.0 nM 6.64
CHEMBL348002 Ki = 237.0 nM 6.62
CHEMBL357532 Ki = 256.0 nM 6.59
CHEMBL346168 Ki = 260.0 nM 6.58
CHEMBL153136 Ki = 267.0 nM 6.57
CHEMBL348014 Ki = 317.0 nM 6.50
CHEMBL347334 Ki = 355.0 nM 6.45
CHEMBL345506 Ki = 386.0 nM 6.41
CHEMBL357286 Ki = 409.0 nM 6.39
CHEMBL348241 Ki = 455.0 nM 6.34
CHEMBL152363 Ki = 669.0 nM 6.17
CHEMBL424332 Ki = 669.0 nM 6.17
CHEMBL347056 Ki = 1000.0 nM 6.00
CHEMBL152311 Ki = 1000.0 nM 6.00
CHEMBL428175 RWJ-25730 Ki = 1006.0 nM 6.00
CHEMBL153219 Ki = 1000.0 nM 6.00
CHEMBL152336 Ki = 1000.0 nM 6.00
CHEMBL346459 Ki > 1000.0 nM -
CHEMBL346881 Ki > 100.0 nM -
CHEMBL153490 Ki > 1000.0 nM -
CHEMBL153263 Ki > 100.0 nM -
CHEMBL9666 Ki > 100.0 nM -
CHEMBL267044 LEVOSULPIRIDE Ki > 1000.0 nM -