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Assay Detail

CHEMBL649341

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

Binding
Binding affinity towards alpha-1 adrenergic receptor using [3H]prazosin as radioligand.
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
Reitz AB, Baxter EW, Bennett DJ, Codd EE, Jordan AD, Malloy EA, Maryanoff BE, McDonnell ME, Ortegon ME, Renzi MJ.
J Med Chem (1995) 38 : 4211 -4222
PubMed 7473548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 8.24 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275045 1 9.15
CHEMBL10085 MAZAPERTINE 2.0 1 8.89
CHEMBL423712 1 8.85
CHEMBL1161079 1 8.77
CHEMBL135135 1 8.74
CHEMBL443546 1 8.72
CHEMBL1161076 1 8.59
CHEMBL134304 1 8.57
CHEMBL1161083 1 8.55
CHEMBL439607 1 8.47
CHEMBL135676 1 8.43
CHEMBL1161126 1 8.40
CHEMBL416703 1 8.40
CHEMBL1161119 1 8.30
CHEMBL422989 1 8.28
CHEMBL135377 1 8.26
CHEMBL1161088 1 8.24
CHEMBL1161087 1 8.24
CHEMBL334767 1 8.24
CHEMBL135246 1 8.21
CHEMBL1161120 1 8.21
CHEMBL135938 1 8.21
CHEMBL1161078 1 8.15
CHEMBL428175 RWJ-25730 1 8.09
CHEMBL135107 1 8.07
CHEMBL341402 1 8.07
CHEMBL1161096 1 8.04
CHEMBL135479 1 7.92
CHEMBL3392290 1 7.89
CHEMBL1161058 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275045 Ki = 0.7 nM 9.15
CHEMBL10085 MAZAPERTINE Ki = 1.3 nM 8.89
CHEMBL423712 Ki = 1.4 nM 8.85
CHEMBL1161079 Ki = 1.7 nM 8.77
CHEMBL135135 Ki = 1.8 nM 8.74
CHEMBL443546 Ki = 1.9 nM 8.72
CHEMBL1161076 Ki = 2.6 nM 8.59
CHEMBL134304 Ki = 2.7 nM 8.57
CHEMBL1161083 Ki = 2.8 nM 8.55
CHEMBL439607 Ki = 3.4 nM 8.47
CHEMBL135676 Ki = 3.7 nM 8.43
CHEMBL1161126 Ki = 4.0 nM 8.40
CHEMBL416703 Ki = 4.0 nM 8.40
CHEMBL1161119 Ki = 5.0 nM 8.30
CHEMBL422989 Ki = 5.3 nM 8.28
CHEMBL135377 Ki = 5.5 nM 8.26
CHEMBL334767 Ki = 5.8 nM 8.24
CHEMBL1161088 Ki = 5.8 nM 8.24
CHEMBL1161087 Ki = 5.7 nM 8.24
CHEMBL135246 Ki = 6.2 nM 8.21
CHEMBL1161120 Ki = 6.2 nM 8.21
CHEMBL135938 Ki = 6.1 nM 8.21
CHEMBL1161078 Ki = 7.1 nM 8.15
CHEMBL428175 RWJ-25730 Ki = 8.2 nM 8.09
CHEMBL135107 Ki = 8.6 nM 8.07
CHEMBL341402 Ki = 8.5 nM 8.07
CHEMBL1161096 Ki = 9.1 nM 8.04
CHEMBL135479 Ki = 12.0 nM 7.92
CHEMBL3392290 Ki = 13.0 nM 7.89
CHEMBL1161058 Ki = 13.0 nM 7.89
CHEMBL340268 Ki = 18.0 nM 7.75
CHEMBL54 HALOPERIDOL Ki = 23.5 nM 7.63
CHEMBL10105 Ki = 32.0 nM 7.50
CHEMBL135129 Ki = 47.0 nM 7.33
CHEMBL135047 Ki = 52.0 nM 7.28
CHEMBL134951 Ki > 1000.0 nM -