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Assay Detail

CHEMBL671944

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

Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Aporphines as antagonists of dopamine D-1 receptors.
Schaus JM, Titus RD, Foreman MM, Mason NR, Truex LL.
J Med Chem (1990) 33 : 600 -607
PubMed 2405158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.06 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62 SCH-23390 1 8.89
CHEMBL119455 1 6.97
CHEMBL155884 1 6.77
CHEMBL155833 1 6.74
CHEMBL53 APOMORPHINE 4.0 1 6.37
CHEMBL153960 1 6.25
CHEMBL345907 1 6.20
CHEMBL157912 (S)-BULBOCAPNINE 1 6.13
CHEMBL154989 1 6.09
CHEMBL117841 1 5.49
CHEMBL345822 1 5.48
CHEMBL416288 (S)APOMORPHINE 1 5.44
CHEMBL157879 1 5.30
CHEMBL346017 1 5.07
CHEMBL155246 1 4.92
CHEMBL154709 APOCIDEINE 1 4.88
CHEMBL157735 1 -
CHEMBL155731 QUINELORANE 2.0 1 -
CHEMBL155883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62 SCH-23390 IC50 = 1.3 nM 8.89
CHEMBL119455 IC50 = 107.0 nM 6.97
CHEMBL155884 IC50 = 171.0 nM 6.77
CHEMBL155833 IC50 = 181.0 nM 6.74
CHEMBL53 APOMORPHINE IC50 = 432.0 nM 6.37
CHEMBL153960 IC50 = 561.0 nM 6.25
CHEMBL345907 IC50 = 637.0 nM 6.20
CHEMBL157912 (S)-BULBOCAPNINE IC50 = 739.0 nM 6.13
CHEMBL154989 IC50 = 818.0 nM 6.09
CHEMBL117841 IC50 = 3276.0 nM 5.49
CHEMBL345822 IC50 = 3340.0 nM 5.48
CHEMBL416288 (S)APOMORPHINE IC50 = 3620.0 nM 5.44
CHEMBL157879 IC50 = 5061.0 nM 5.30
CHEMBL346017 IC50 = 8611.0 nM 5.07
CHEMBL155246 IC50 = 12100.0 nM 4.92
CHEMBL154709 APOCIDEINE IC50 = 13300.0 nM 4.88
CHEMBL157735 IC50 > 1000.0 nM -
CHEMBL155731 QUINELORANE IC50 > 10000.0 nM -
CHEMBL155883 IC50 > 1000.0 nM -