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Assay Detail

CHEMBL944160

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

Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptor
72
Total Activities
69
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Advances in development of dopaminergic aporphinoids.
Zhang A, Zhang Y, Branfman AR, Baldessarini RJ, Neumeyer JL.
J Med Chem (2007) 50 : 171 -181
PubMed 17228858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 5.90 8.70
IC50 25 5.61 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256075 1 8.70
CHEMBL401690 1 8.22
CHEMBL401689 1 7.82
CHEMBL225853 3-BROMOBOLDINE 1 7.31
CHEMBL452776 CELTISINE 1 7.22
CHEMBL452510 BREOGANINE 1 7.00
CHEMBL119455 1 6.96
CHEMBL155884 1 6.77
CHEMBL404137 1 6.77
CHEMBL53 APOMORPHINE 4.0 1 6.68
CHEMBL404136 PREDICENTRINE 1 6.62
CHEMBL118254 1 6.57
CHEMBL388342 BOLDINE 2 6.54
CHEMBL53510 1 6.42
CHEMBL258370 PUKATEINE 1 6.40
CHEMBL403032 1 6.28
CHEMBL27559 1 6.16
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 6.14
CHEMBL157912 (S)-BULBOCAPNINE 1 6.13
CHEMBL258372 1 6.10
CHEMBL455633 CULARIDINE 1 6.10
CHEMBL288096 2 6.04
CHEMBL322574 1 6.01
CHEMBL452512 CLAVICULINE 1 6.00
CHEMBL332332 1 5.96
CHEMBL106622 1 5.89
CHEMBL283489 1 5.85
CHEMBL53294 2 5.75
CHEMBL119593 1 5.70
CHEMBL401567 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256075 Ki = 2.0 nM 8.70
CHEMBL401690 Ki = 6.0 nM 8.22
CHEMBL401689 Ki = 15.0 nM 7.82
CHEMBL225853 3-BROMOBOLDINE Ki = 49.0 nM 7.31
CHEMBL452776 CELTISINE IC50 = 60.0 nM 7.22
CHEMBL452510 BREOGANINE IC50 = 100.0 nM 7.00
CHEMBL119455 IC50 = 110.0 nM 6.96
CHEMBL155884 IC50 = 170.0 nM 6.77
CHEMBL404137 Ki = 170.0 nM 6.77
CHEMBL53 APOMORPHINE Ki = 210.0 nM 6.68
CHEMBL404136 PREDICENTRINE Ki = 240.0 nM 6.62
CHEMBL118254 Ki = 270.0 nM 6.57
CHEMBL388342 BOLDINE Ki = 290.0 nM 6.54
CHEMBL53510 Ki = 380.0 nM 6.42
CHEMBL258370 PUKATEINE IC50 = 400.0 nM 6.40
CHEMBL388342 BOLDINE IC50 = 400.0 nM 6.40
CHEMBL403032 Ki = 520.0 nM 6.28
CHEMBL27559 Ki = 700.0 nM 6.16
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 730.0 nM 6.14
CHEMBL157912 (S)-BULBOCAPNINE IC50 = 740.0 nM 6.13
CHEMBL258372 Ki = 800.0 nM 6.10
CHEMBL455633 CULARIDINE IC50 = 800.0 nM 6.10
CHEMBL288096 Ki = 920.0 nM 6.04
CHEMBL322574 IC50 = 970.0 nM 6.01
CHEMBL452512 CLAVICULINE IC50 = 1000.0 nM 6.00
CHEMBL332332 Ki = 1100.0 nM 5.96
CHEMBL106622 IC50 = 1300.0 nM 5.89
CHEMBL283489 Ki = 1413.0 nM 5.85
CHEMBL288096 IC50 = 1720.0 nM 5.76
CHEMBL53294 Ki = 1800.0 nM 5.75
CHEMBL119593 Ki = 2000.0 nM 5.70
CHEMBL401567 Ki = 2110.0 nM 5.68
CHEMBL487388 NORBOLDINE IC50 = 2500.0 nM 5.60
CHEMBL228082 GLAUCINE Ki = 2900.0 nM 5.54
CHEMBL155208 Ki = 3000.0 nM 5.52
CHEMBL53294 IC50 = 3300.0 nM 5.48
CHEMBL439639 Ki = 3500.0 nM 5.46
CHEMBL253530 Ki = 3700.0 nM 5.43
CHEMBL254147 Ki = 4300.0 nM 5.37
CHEMBL257745 NORSTEPHALAGINE IC50 = 4800.0 nM 5.32
CHEMBL155352 Ki = 4800.0 nM 5.32
CHEMBL253738 Ki = 6100.0 nM 5.21
CHEMBL402736 Ki = 6300.0 nM 5.20
CHEMBL404865 Ki = 6400.0 nM 5.19
CHEMBL253736 Ki = 6600.0 nM 5.18
CHEMBL154468 Ki = 6800.0 nM 5.17
CHEMBL404240 Ki = 7200.0 nM 5.14
CHEMBL253947 Ki = 8300.0 nM 5.08
CHEMBL402735 Ki = 8600.0 nM 5.07
CHEMBL508011 ISOPILINE IC50 = 9800.0 nM 5.01