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Assay Detail

CHEMBL645698

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

Binding
The compound was tested for its binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortex
34
Total Activities
34
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

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 34 7.32 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434512 1 8.28
CHEMBL345506 1 8.14
CHEMBL428175 RWJ-25730 1 8.09
CHEMBL347334 1 7.95
CHEMBL348002 1 7.80
CHEMBL152311 1 7.79
CHEMBL153136 1 7.76
CHEMBL357286 1 7.70
CHEMBL346168 1 7.68
CHEMBL347056 1 7.64
CHEMBL348014 1 7.58
CHEMBL348241 1 7.56
CHEMBL422 TRIFLUOPERAZINE 4.0 1 7.53
CHEMBL347782 1 7.45
CHEMBL153335 1 7.42
CHEMBL152336 1 7.37
CHEMBL153490 1 7.35
CHEMBL267777 RITANSERIN 2.0 1 7.30
CHEMBL152867 1 7.28
CHEMBL152458 1 7.27
CHEMBL152204 1 7.20
CHEMBL152424 1 7.00
CHEMBL151966 1 6.87
CHEMBL49 BUSPIRONE 4.0 1 6.86
CHEMBL152617 1 6.85
CHEMBL152776 1 6.78
CHEMBL357532 1 6.58
CHEMBL346459 1 6.36
CHEMBL9666 1 6.29
CHEMBL153161 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434512 Ki = 5.2 nM 8.28
CHEMBL345506 Ki = 7.3 nM 8.14
CHEMBL428175 RWJ-25730 Ki = 8.2 nM 8.09
CHEMBL347334 Ki = 11.3 nM 7.95
CHEMBL348002 Ki = 15.7 nM 7.80
CHEMBL152311 Ki = 16.3 nM 7.79
CHEMBL153136 Ki = 17.4 nM 7.76
CHEMBL357286 Ki = 20.0 nM 7.70
CHEMBL346168 Ki = 20.8 nM 7.68
CHEMBL347056 Ki = 23.1 nM 7.64
CHEMBL348014 Ki = 26.6 nM 7.58
CHEMBL348241 Ki = 27.5 nM 7.56
CHEMBL422 TRIFLUOPERAZINE Ki = 29.3 nM 7.53
CHEMBL347782 Ki = 35.9 nM 7.45
CHEMBL153335 Ki = 38.2 nM 7.42
CHEMBL152336 Ki = 43.1 nM 7.37
CHEMBL153490 Ki = 44.9 nM 7.35
CHEMBL267777 RITANSERIN Ki = 49.5 nM 7.30
CHEMBL152867 Ki = 53.1 nM 7.28
CHEMBL152458 Ki = 53.9 nM 7.27
CHEMBL152204 Ki = 63.7 nM 7.20
CHEMBL152424 Ki = 100.0 nM 7.00
CHEMBL151966 Ki = 136.0 nM 6.87
CHEMBL49 BUSPIRONE Ki = 138.0 nM 6.86
CHEMBL152617 Ki = 140.0 nM 6.85
CHEMBL152776 Ki = 166.0 nM 6.78
CHEMBL357532 Ki = 264.0 nM 6.58
CHEMBL346459 Ki = 436.0 nM 6.36
CHEMBL9666 Ki = 510.0 nM 6.29
CHEMBL153161 Ki = 1000.0 nM 6.00
CHEMBL153263 Ki > 100.0 nM -
CHEMBL267044 LEVOSULPIRIDE Ki > 1000.0 nM -
CHEMBL346881 Ki > 100.0 nM -
CHEMBL153219 Ki > 1000.0 nM -