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Assay Detail

CHEMBL4345332

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

Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL ↗
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
Park H, Urs AN, Zimmerman J, Liu C, Wang Q, Urs NM.
ACS Med Chem Lett (2020) 11 : 385 -392
PubMed 32184974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 7.29 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE — 2 10.40
CHEMBL4555547 — — 2 9.43
CHEMBL53 APOMORPHINE 4.0 2 8.80
CHEMBL4470553 — — 2 8.11
CHEMBL3276140 — — 2 7.90
CHEMBL4523054 — — 2 6.24
CHEMBL4550010 — — 2 5.83
CHEMBL4568388 — — 2 5.72
CHEMBL4437552 — — 2 5.45
CHEMBL4591021 — — 2 5.08
CHEMBL4467483 — — 2 -
CHEMBL4564103 — — 2 -
CHEMBL4579687 — — 2 -
CHEMBL4513262 — — 2 -
CHEMBL4439029 — — 2 -
CHEMBL35426 — — 2 -
CHEMBL4442011 — — 2 -
CHEMBL4435882 — — 2 -
CHEMBL4537900 — — 2 -
CHEMBL4589737 — — 2 -
CHEMBL4438800 — — 2 -
CHEMBL4581262 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE EC50 = 0.03981 nM 10.40
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE EC50 = 0.04 nM 10.40
CHEMBL4555547 — EC50 = 0.373 nM 9.43
CHEMBL4555547 — EC50 = 0.3715 nM 9.43
CHEMBL53 APOMORPHINE EC50 = 1.585 nM 8.80
CHEMBL53 APOMORPHINE EC50 = 1.61 nM 8.79
CHEMBL4470553 — EC50 = 7.7 nM 8.11
CHEMBL4470553 — EC50 = 7.762 nM 8.11
CHEMBL3276140 — EC50 = 12.59 nM 7.90
CHEMBL3276140 — EC50 = 12.86 nM 7.89
CHEMBL4523054 — EC50 = 575.44 nM 6.24
CHEMBL4523054 — EC50 = 579.7 nM 6.24
CHEMBL4550010 — EC50 = 1496.0 nM 5.83
CHEMBL4550010 — EC50 = 1584.89 nM 5.80
CHEMBL4568388 — EC50 = 1913.0 nM 5.72
CHEMBL4568388 — EC50 = 1995.26 nM 5.70
CHEMBL4437552 — EC50 = 3548.13 nM 5.45
CHEMBL4437552 — EC50 = 3586.0 nM 5.45
CHEMBL4591021 — EC50 = 8317.64 nM 5.08
CHEMBL4591021 — EC50 = 8236.0 nM 5.08
CHEMBL4581262 — EC50 > 10000.0 nM -
CHEMBL4537900 — EC50 > 10000.0 nM -
CHEMBL4435882 — EC50 > 10000.0 nM -
CHEMBL35426 — EC50 > 10000.0 nM -
CHEMBL4589737 — EC50 > 10000.0 nM -
CHEMBL4442011 — EC50 > 10000.0 nM -
CHEMBL4439029 — EC50 > 10000.0 nM -
CHEMBL4513262 — EC50 > 10000.0 nM -
CHEMBL4467483 — EC50 > 10000.0 nM -
CHEMBL4564103 — EC50 > 10000.0 nM -
CHEMBL4579687 — EC50 > 10000.0 nM -
CHEMBL4438800 — EC50 > 10000.0 nM -
CHEMBL4439029 — EC50 > 10000.0 nM -
CHEMBL4442011 — EC50 > 10000.0 nM -
CHEMBL4589737 — EC50 > 10000.0 nM -
CHEMBL4467483 — EC50 > 10000.0 nM -
CHEMBL4564103 — EC50 > 10000.0 nM -
CHEMBL4579687 — EC50 > 10000.0 nM -
CHEMBL35426 — EC50 > 10000.0 nM -
CHEMBL4435882 — EC50 > 10000.0 nM -
CHEMBL4537900 — EC50 > 10000.0 nM -
CHEMBL4581262 — EC50 > 10000.0 nM -
CHEMBL4513262 — EC50 > 10000.0 nM -
CHEMBL4438800 — EC50 > 10000.0 nM -