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Assay Detail

CHEMBL673004

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

Binding
Inhibition of [3H]spiroperidol (0.5 nM) binding to dopamine receptor from rat striatal membrane.
33
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
Sarges R, Howard HR, Donahue KM, Welch WM, Dominy BW, Weissman A, Koe BK, Bordner J.
J Med Chem (1986) 29 : 8 -19
PubMed 3941416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.40 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542376 1 8.24
CHEMBL553243 1 8.22
CHEMBL417401 1 8.17
CHEMBL539257 1 8.12
CHEMBL542375 1 8.07
CHEMBL545436 1 8.03
CHEMBL57241 FLUTROLINE 2.0 1 7.92
CHEMBL545209 1 7.92
CHEMBL299903 1 7.92
CHEMBL543095 1 7.89
CHEMBL543327 1 7.89
CHEMBL540282 1 7.85
CHEMBL294488 1 7.85
CHEMBL544039 1 7.72
CHEMBL60634 2 7.66
CHEMBL57351 2 7.60
CHEMBL544036 1 7.60
CHEMBL294025 1 7.58
CHEMBL56580 1 7.46
CHEMBL538242 1 7.35
CHEMBL552625 1 7.27
CHEMBL47050 PENFLURIDOL 2.0 1 7.21
CHEMBL543569 1 7.17
CHEMBL553953 1 7.08
CHEMBL542858 1 6.85
CHEMBL292214 1 6.66
CHEMBL59582 1 6.46
CHEMBL543325 1 6.00
CHEMBL55545 1 5.50
CHEMBL538990 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542376 IC50 = 5.8 nM 8.24
CHEMBL553243 IC50 = 6.0 nM 8.22
CHEMBL417401 IC50 = 6.7 nM 8.17
CHEMBL539257 IC50 = 7.5 nM 8.12
CHEMBL542375 IC50 = 8.5 nM 8.07
CHEMBL545436 IC50 = 9.4 nM 8.03
CHEMBL545209 IC50 = 12.0 nM 7.92
CHEMBL57241 FLUTROLINE IC50 = 12.0 nM 7.92
CHEMBL299903 IC50 = 12.0 nM 7.92
CHEMBL543095 IC50 = 13.0 nM 7.89
CHEMBL543327 IC50 = 13.0 nM 7.89
CHEMBL540282 IC50 = 14.0 nM 7.85
CHEMBL294488 IC50 = 14.0 nM 7.85
CHEMBL544039 IC50 = 19.0 nM 7.72
CHEMBL60634 IC50 = 22.0 nM 7.66
CHEMBL57351 IC50 = 25.0 nM 7.60
CHEMBL544036 IC50 = 25.0 nM 7.60
CHEMBL294025 IC50 = 26.0 nM 7.58
CHEMBL56580 IC50 = 35.0 nM 7.46
CHEMBL538242 IC50 = 45.0 nM 7.35
CHEMBL552625 IC50 = 54.0 nM 7.27
CHEMBL47050 PENFLURIDOL IC50 = 62.0 nM 7.21
CHEMBL543569 IC50 = 68.0 nM 7.17
CHEMBL553953 IC50 = 83.0 nM 7.08
CHEMBL542858 IC50 = 140.0 nM 6.85
CHEMBL292214 IC50 = 220.0 nM 6.66
CHEMBL59582 IC50 = 350.0 nM 6.46
CHEMBL57351 IC50 = 350.0 nM 6.46
CHEMBL543325 IC50 = 1000.0 nM 6.00
CHEMBL60634 IC50 = 1800.0 nM 5.75
CHEMBL55545 IC50 = 3200.0 nM 5.50
CHEMBL538990 IC50 > 1000.0 nM -
CHEMBL544741 IC50 > 320.0 nM -