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Assay Detail

CHEMBL4345330

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Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL ↗
40
Total Activities
20
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(1A) dopamine receptor (CHEMBL2056) ↗
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 40 6.82 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE — 2 8.96
CHEMBL53 APOMORPHINE 4.0 2 8.42
CHEMBL3276140 — — 2 7.69
CHEMBL4555547 — — 2 7.50
CHEMBL4589737 — — 2 7.06
CHEMBL35426 — — 2 7.00
CHEMBL4579687 — — 2 6.82
CHEMBL4581262 — — 2 6.71
CHEMBL4467483 — — 2 6.62
CHEMBL4438800 — — 2 6.48
CHEMBL4513262 — — 2 6.41
CHEMBL4442011 — — 2 6.30
CHEMBL4435882 — — 2 6.18
CHEMBL4470553 — — 2 6.14
CHEMBL4537900 — — 2 6.02
CHEMBL4437552 — — 2 5.81
CHEMBL4523054 — — 2 5.81
CHEMBL4591021 — — 2 -
CHEMBL4439029 — — 2 -
CHEMBL4564103 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE EC50 = 1.1 nM 8.96
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE EC50 = 1.096 nM 8.96
CHEMBL53 APOMORPHINE EC50 = 3.77 nM 8.42
CHEMBL53 APOMORPHINE EC50 = 3.981 nM 8.40
CHEMBL3276140 — EC50 = 20.4 nM 7.69
CHEMBL3276140 — EC50 = 20.42 nM 7.69
CHEMBL4555547 — EC50 = 31.7 nM 7.50
CHEMBL4555547 — EC50 = 31.62 nM 7.50
CHEMBL4589737 — EC50 = 87.1 nM 7.06
CHEMBL4589737 — EC50 = 87.44 nM 7.06
CHEMBL35426 — EC50 = 100.0 nM 7.00
CHEMBL35426 — EC50 = 112.2 nM 6.95
CHEMBL4579687 — EC50 = 151.36 nM 6.82
CHEMBL4579687 — EC50 = 150.2 nM 6.82
CHEMBL4581262 — EC50 = 194.3 nM 6.71
CHEMBL4581262 — EC50 = 194.98 nM 6.71
CHEMBL4467483 — EC50 = 239.2 nM 6.62
CHEMBL4467483 — EC50 = 239.88 nM 6.62
CHEMBL4438800 — EC50 = 333.9 nM 6.48
CHEMBL4438800 — EC50 = 354.81 nM 6.45
CHEMBL4513262 — EC50 = 389.05 nM 6.41
CHEMBL4513262 — EC50 = 385.9 nM 6.41
CHEMBL4442011 — EC50 = 501.19 nM 6.30
CHEMBL4442011 — EC50 = 505.1 nM 6.30
CHEMBL4435882 — EC50 = 660.69 nM 6.18
CHEMBL4435882 — EC50 = 669.1 nM 6.17
CHEMBL4470553 — EC50 = 717.5 nM 6.14
CHEMBL4470553 — EC50 = 724.44 nM 6.14
CHEMBL4537900 — EC50 = 951.4 nM 6.02
CHEMBL4537900 — EC50 = 954.99 nM 6.02
CHEMBL4523054 — EC50 = 1548.82 nM 5.81
CHEMBL4437552 — EC50 = 1548.0 nM 5.81
CHEMBL4523054 — EC50 = 1555.0 nM 5.81
CHEMBL4437552 — EC50 = 1548.82 nM 5.81
CHEMBL4439029 — EC50 > 10000.0 nM -
CHEMBL4564103 — EC50 > 10000.0 nM -
CHEMBL4439029 — EC50 > 10000.0 nM -
CHEMBL4591021 — EC50 > 10000.0 nM -
CHEMBL4564103 — EC50 > 10000.0 nM -
CHEMBL4591021 — EC50 > 10000.0 nM -