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Assay Detail

CHEMBL672372

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Binding
In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes.
22
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6 glioma
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.
Wilcox RE, Huang WH, Brusniak MY, Wilcox DM, Pearlman RS, Teeter MM, DuRand CJ, Wiens BL, Neve KA.
J Med Chem (2000) 43 : 3005 -3019
PubMed 10956209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 22 6.67 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 9.22
CHEMBL227213 2 9.21
CHEMBL493 BROMOCRIPTINE 4.0 1 8.10
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 8.05
CHEMBL612083 1 8.00
CHEMBL531 PERGOLIDE 4.0 1 7.52
CHEMBL53 APOMORPHINE 4.0 1 6.70
CHEMBL1160788 1 6.68
CHEMBL104141 2 6.52
CHEMBL317741 1 6.40
CHEMBL301559 1 6.40
CHEMBL34095 1 6.32
CHEMBL588 FENOLDOPAM 4.0 1 5.89
CHEMBL240773 QUINPIROLE 2.0 1 5.72
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.64
CHEMBL1160787 2 5.52
CHEMBL59 DOPAMINE 4.0 1 5.21
CHEMBL286080 SKF-38393 1 4.34
CHEMBL1160785 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Kd = 0.6 nM 9.22
CHEMBL227213 Kd = 0.62 nM 9.21
CHEMBL227213 Kd = 0.62 nM 9.21
CHEMBL493 BROMOCRIPTINE Kd = 8.0 nM 8.10
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Kd = 9.0 nM 8.05
CHEMBL612083 Kd = 10.0 nM 8.00
CHEMBL531 PERGOLIDE Kd = 30.0 nM 7.52
CHEMBL53 APOMORPHINE Kd = 200.0 nM 6.70
CHEMBL1160788 Kd = 210.0 nM 6.68
CHEMBL104141 Kd = 300.0 nM 6.52
CHEMBL104141 Kd = 300.0 nM 6.52
CHEMBL317741 Kd = 400.0 nM 6.40
CHEMBL301559 Kd = 400.0 nM 6.40
CHEMBL34095 Kd = 480.0 nM 6.32
CHEMBL588 FENOLDOPAM Kd = 1300.0 nM 5.89
CHEMBL240773 QUINPIROLE Kd = 1900.0 nM 5.72
CHEMBL25856 DIHYDREXIDINE Kd = 2300.0 nM 5.64
CHEMBL1160787 Kd = 3000.0 nM 5.52
CHEMBL1160787 Kd = 3000.0 nM 5.52
CHEMBL59 DOPAMINE Kd = 6200.0 nM 5.21
CHEMBL286080 SKF-38393 Kd = 46000.0 nM 4.34
CHEMBL1160785 Kd = 94000.0 nM 4.03