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Assay Detail

CHEMBL671494

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

Binding
Binding affinity against D2 receptor in rat corpus striatum using [3H]sulpiride as the radioligand
46
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site.
Mewshaw RE, Sherrill RG, Mathew RM, Kaiser C, Bailey MA, Karbon EW.
J Med Chem (1993) 36 : 343 -352
PubMed 8426363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 46 5.70 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442395 1 8.22
CHEMBL119047 1 7.00
CHEMBL36645 1 6.57
CHEMBL117898 4 6.48
CHEMBL324092 1 6.28
CHEMBL119867 1 6.21
CHEMBL118289 1 6.19
CHEMBL332035 1 6.17
CHEMBL325845 1 6.15
CHEMBL38130 1 6.13
CHEMBL35711 1 6.11
CHEMBL119804 1 6.08
CHEMBL38152 1 5.94
CHEMBL119048 1 5.89
CHEMBL433022 1 5.80
CHEMBL118665 1 5.79
CHEMBL116711 1 5.75
CHEMBL331500 1 5.74
CHEMBL119075 1 5.74
CHEMBL116207 1 5.70
CHEMBL119811 1 5.68
CHEMBL115582 1 5.65
CHEMBL117567 1 5.62
CHEMBL119485 1 5.61
CHEMBL116710 1 5.60
CHEMBL119889 1 5.58
CHEMBL332593 1 5.58
CHEMBL333840 1 5.58
CHEMBL285203 1 5.52
CHEMBL325619 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442395 Ki = 6.0 nM 8.22
CHEMBL119047 Ki = 100.0 nM 7.00
CHEMBL36645 Ki = 270.0 nM 6.57
CHEMBL117898 Ki = 330.0 nM 6.48
CHEMBL324092 Ki = 530.0 nM 6.28
CHEMBL119867 Ki = 620.0 nM 6.21
CHEMBL118289 Ki = 650.0 nM 6.19
CHEMBL332035 Ki = 677.0 nM 6.17
CHEMBL325845 Ki = 710.0 nM 6.15
CHEMBL38130 Ki = 733.0 nM 6.13
CHEMBL35711 Ki = 769.0 nM 6.11
CHEMBL119804 Ki = 840.0 nM 6.08
CHEMBL38152 Ki = 1160.0 nM 5.94
CHEMBL117898 Ki = 1270.0 nM 5.90
CHEMBL117898 Ki = 1270.0 nM 5.90
CHEMBL119048 Ki = 1280.0 nM 5.89
CHEMBL433022 Ki = 1570.0 nM 5.80
CHEMBL118665 Ki = 1620.0 nM 5.79
CHEMBL116711 Ki = 1780.0 nM 5.75
CHEMBL119075 Ki = 1820.0 nM 5.74
CHEMBL331500 Ki = 1830.0 nM 5.74
CHEMBL116207 Ki = 2000.0 nM 5.70
CHEMBL119811 Ki = 2100.0 nM 5.68
CHEMBL115582 Ki = 2230.0 nM 5.65
CHEMBL117567 Ki = 2420.0 nM 5.62
CHEMBL119485 Ki = 2460.0 nM 5.61
CHEMBL116710 Ki = 2530.0 nM 5.60
CHEMBL332593 Ki = 2600.0 nM 5.58
CHEMBL333840 Ki = 2600.0 nM 5.58
CHEMBL119889 Ki = 2640.0 nM 5.58
CHEMBL285203 Ki = 3000.0 nM 5.52
CHEMBL117898 Ki = 3150.0 nM 5.50
CHEMBL325619 Ki = 3430.0 nM 5.46
CHEMBL118288 Ki = 3650.0 nM 5.44
CHEMBL117748 Ki = 3790.0 nM 5.42
CHEMBL331611 Ki = 4520.0 nM 5.34
CHEMBL323910 Ki = 5310.0 nM 5.28
CHEMBL118445 Ki = 10000.0 nM 5.00
CHEMBL119495 Ki = 11200.0 nM 4.95
CHEMBL325168 Ki = 12200.0 nM 4.91
CHEMBL119725 Ki = 12300.0 nM 4.91
CHEMBL118276 Ki = 16600.0 nM 4.78
CHEMBL331006 Ki = 36600.0 nM 4.44
CHEMBL119409 Ki = 37300.0 nM 4.43
CHEMBL119698 Ki = 52100.0 nM 4.28
CHEMBL117695 Ki > 10000.0 nM -