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Assay Detail

CHEMBL4394476

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

ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assay
ChEMBL ↗
54
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

D<sub>2</sub> Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine.
Shen Y, McCorvy JD, Martini ML, Rodriguiz RM, Pogorelov VM, Ward KM, Wetsel WC, Liu J, Roth BL, Jin J.
J Med Chem (2019) 62 : 4755 -4771
PubMed 30964661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 51 7.54 9.22
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 2 9.22
CHEMBL4526364 — — 2 8.71
CHEMBL4467173 — — 2 8.70
CHEMBL240773 QUINPIROLE 2.0 2 8.57
CHEMBL4457507 — — 2 8.40
CHEMBL4446533 — — 2 8.32
CHEMBL3085821 — — 2 8.05
CHEMBL4470060 — — 2 8.00
CHEMBL3085826 — — 2 7.93
CHEMBL4517517 — — 2 7.78
CHEMBL4441636 — — 2 7.59
CHEMBL4451797 — — 2 7.40
CHEMBL4460025 — — 2 7.27
CHEMBL4532767 — — 2 7.22
CHEMBL4437205 — — 2 7.19
CHEMBL3085802 — — 2 7.16
CHEMBL4447058 — — 2 7.06
CHEMBL4587909 — — 2 6.74
CHEMBL3088209 — — 2 6.71
CHEMBL4448960 — — 2 6.70
CHEMBL3088212 — — 2 6.62
CHEMBL4465281 — — 2 6.51
CHEMBL3088211 — — 2 6.20
CHEMBL3085816 — — 2 -
CHEMBL4458270 — — 2 -
CHEMBL4593504 — — 2 -
CHEMBL4439118 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE EC50 = 0.6 nM 9.22
CHEMBL2028019 CARIPRAZINE EC50 = 0.631 nM 9.20
CHEMBL4526364 — EC50 = 1.95 nM 8.71
CHEMBL4526364 — EC50 = 2.0 nM 8.70
CHEMBL4467173 — EC50 = 2.0 nM 8.70
CHEMBL4467173 — EC50 = 2.399 nM 8.62
CHEMBL240773 QUINPIROLE EC50 = 2.692 nM 8.57
CHEMBL4457507 — EC50 = 4.0 nM 8.40
CHEMBL4457507 — EC50 = 4.074 nM 8.39
CHEMBL4446533 — EC50 = 4.786 nM 8.32
CHEMBL4446533 — EC50 = 5.0 nM 8.30
CHEMBL3085821 — EC50 = 9.0 nM 8.05
CHEMBL3085821 — EC50 = 9.12 nM 8.04
CHEMBL4470060 — EC50 = 10.0 nM 8.00
CHEMBL4470060 — EC50 = 10.47 nM 7.98
CHEMBL3085826 — EC50 = 11.75 nM 7.93
CHEMBL3085826 — EC50 = 12.0 nM 7.92
CHEMBL4517517 — EC50 = 16.6 nM 7.78
CHEMBL4517517 — EC50 = 17.0 nM 7.77
CHEMBL4441636 — EC50 = 25.7 nM 7.59
CHEMBL4441636 — EC50 = 26.0 nM 7.58
CHEMBL4451797 — EC50 = 40.0 nM 7.40
CHEMBL4451797 — EC50 = 40.74 nM 7.39
CHEMBL4460025 — EC50 = 54.0 nM 7.27
CHEMBL4460025 — EC50 = 53.7 nM 7.27
CHEMBL4532767 — EC50 = 60.0 nM 7.22
CHEMBL4532767 — EC50 = 60.26 nM 7.22
CHEMBL4437205 — EC50 = 65.0 nM 7.19
CHEMBL4437205 — EC50 = 64.57 nM 7.19
CHEMBL3085802 — EC50 = 69.18 nM 7.16
CHEMBL3085802 — EC50 = 69.0 nM 7.16
CHEMBL4447058 — EC50 = 88.0 nM 7.06
CHEMBL4447058 — EC50 = 89.13 nM 7.05
CHEMBL4587909 — EC50 = 183.0 nM 6.74
CHEMBL4587909 — EC50 = 181.97 nM 6.74
CHEMBL3088209 — EC50 = 194.98 nM 6.71
CHEMBL3088209 — EC50 = 195.0 nM 6.71
CHEMBL4448960 — EC50 = 202.0 nM 6.70
CHEMBL4448960 — EC50 = 204.17 nM 6.69
CHEMBL3088212 — EC50 = 239.88 nM 6.62
CHEMBL3088212 — EC50 = 238.0 nM 6.62
CHEMBL4465281 — EC50 = 312.0 nM 6.51
CHEMBL4465281 — EC50 = 309.03 nM 6.51
CHEMBL3088211 — EC50 = 636.0 nM 6.20
CHEMBL3088211 — EC50 = 630.96 nM 6.20
CHEMBL4439118 — pEC50 - — -
CHEMBL4593504 — pEC50 - — -
CHEMBL4458270 — pEC50 - — -
CHEMBL3085816 — EC50 > 1000.0 nM -
CHEMBL4439118 — EC50 - — -