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Assay Detail

CHEMBL831909

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

Binding
Displacement of [3H]spiperone from dopamine D2 receptor of rat striatal membranes
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Indolebutylamines as selective 5-HT(1A) agonists.
Heinrich T, Böttcher H, Bartoszyk GD, Greiner HE, Seyfried CA, Van Amsterdam C.
J Med Chem (2004) 47 : 4677 -4683
PubMed 15341483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.30 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185860 — — 1 8.92
CHEMBL362771 — — 1 8.38
CHEMBL186423 — — 1 8.30
CHEMBL431367 ROXINDOLE 2.0 1 8.25
CHEMBL189450 — — 1 8.21
CHEMBL365716 — — 1 8.15
CHEMBL188625 — — 1 7.77
CHEMBL130327 — — 1 7.70
CHEMBL363537 — — 1 7.66
CHEMBL360179 — — 1 7.55
CHEMBL188183 — — 1 7.51
CHEMBL186229 — — 1 7.50
CHEMBL364592 — — 1 7.40
CHEMBL186173 — — 1 7.28
CHEMBL363932 — — 1 7.10
CHEMBL186608 — — 1 7.01
CHEMBL364181 — — 1 7.00
CHEMBL366271 — — 1 7.00
CHEMBL186409 — — 1 7.00
CHEMBL186034 — — 1 6.95
CHEMBL188296 — — 1 6.92
CHEMBL360419 — — 1 6.85
CHEMBL439664 — — 1 6.81
CHEMBL188408 — — 1 6.66
CHEMBL185779 — — 1 6.52
CHEMBL187196 — — 1 6.38
CHEMBL188184 — — 1 6.00
CHEMBL8412 IPSAPIRONE 2.0 1 5.54
CHEMBL426616 — — 1 -
CHEMBL359793 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185860 — IC50 = 1.2 nM 8.92
CHEMBL362771 — IC50 = 4.2 nM 8.38
CHEMBL186423 — IC50 = 5.0 nM 8.30
CHEMBL431367 ROXINDOLE IC50 = 5.6 nM 8.25
CHEMBL189450 — IC50 = 6.2 nM 8.21
CHEMBL365716 — IC50 = 7.0 nM 8.15
CHEMBL188625 — IC50 = 17.0 nM 7.77
CHEMBL130327 — IC50 = 20.0 nM 7.70
CHEMBL363537 — IC50 = 22.0 nM 7.66
CHEMBL360179 — IC50 = 28.0 nM 7.55
CHEMBL188183 — IC50 = 31.0 nM 7.51
CHEMBL186229 — IC50 = 32.0 nM 7.50
CHEMBL364592 — IC50 = 40.0 nM 7.40
CHEMBL186173 — IC50 = 53.0 nM 7.28
CHEMBL363932 — IC50 = 80.0 nM 7.10
CHEMBL186608 — IC50 = 97.0 nM 7.01
CHEMBL364181 — IC50 = 100.0 nM 7.00
CHEMBL366271 — IC50 = 100.0 nM 7.00
CHEMBL186409 — IC50 = 100.0 nM 7.00
CHEMBL186034 — IC50 = 113.0 nM 6.95
CHEMBL188296 — IC50 = 120.0 nM 6.92
CHEMBL360419 — IC50 = 140.0 nM 6.85
CHEMBL439664 — IC50 = 156.0 nM 6.81
CHEMBL188408 — IC50 = 220.0 nM 6.66
CHEMBL185779 — IC50 = 300.0 nM 6.52
CHEMBL187196 — IC50 = 420.0 nM 6.38
CHEMBL188184 — IC50 = 1000.0 nM 6.00
CHEMBL8412 IPSAPIRONE IC50 = 2900.0 nM 5.54
CHEMBL189454 — IC50 > 100.0 nM -
CHEMBL364150 — IC50 > 100.0 nM -
CHEMBL185899 — IC50 > 100.0 nM -
CHEMBL188674 — IC50 > 100.0 nM -
CHEMBL434899 — IC50 > 100.0 nM -
CHEMBL364341 — IC50 > 100.0 nM -
CHEMBL186415 — IC50 > 100.0 nM -
CHEMBL186115 — IC50 > 100.0 nM -
CHEMBL360415 — IC50 > 100.0 nM -
CHEMBL366269 — IC50 > 100.0 nM -
CHEMBL363292 — IC50 > 100.0 nM -
CHEMBL185915 — IC50 > 100.0 nM -
CHEMBL188471 — IC50 > 100.0 nM -
CHEMBL365433 — IC50 > 100.0 nM -
CHEMBL185938 — IC50 > 850.0 nM -
CHEMBL189708 — IC50 > 100.0 nM -
CHEMBL186814 — IC50 > 100.0 nM -
CHEMBL366104 — IC50 > 100.0 nM -
CHEMBL186405 — IC50 ~ 100.0 nM -
CHEMBL359793 — IC50 > 100.0 nM -
CHEMBL426616 — IC50 > 100.0 nM -