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Assay Detail

CHEMBL4394473

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

Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL ↗
62
Total Activities
31
Compounds Tested
2
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

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 59 7.79 9.40
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 2 9.40
CHEMBL4526364 — — 2 9.19
CHEMBL240773 QUINPIROLE 2.0 2 8.74
CHEMBL4467173 — — 2 8.58
CHEMBL4457507 — — 2 8.55
CHEMBL3085826 — — 2 8.52
CHEMBL4517517 — — 2 8.30
CHEMBL4470060 — — 2 8.17
CHEMBL4437205 — — 2 8.12
CHEMBL4446533 — — 2 8.10
CHEMBL4441636 — — 2 8.01
CHEMBL4451797 — — 2 7.97
CHEMBL3085802 — — 2 7.92
CHEMBL3085821 — — 2 7.85
CHEMBL4447058 — — 2 7.85
CHEMBL4460025 — — 2 7.72
CHEMBL4532767 — — 2 7.57
CHEMBL3088209 — — 2 7.48
CHEMBL4465281 — — 2 7.33
CHEMBL3088210 — — 2 7.27
CHEMBL4590026 — — 2 7.17
CHEMBL4587909 — — 2 7.15
CHEMBL3088212 — — 2 7.13
CHEMBL4448960 — — 2 7.07
CHEMBL4473178 — — 2 6.89
CHEMBL4461089 — — 2 6.88
CHEMBL3088211 — — 2 6.84
CHEMBL3085816 — — 2 6.59
CHEMBL4458270 — — 2 -
CHEMBL4593504 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE EC50 = 0.4 nM 9.40
CHEMBL2028019 CARIPRAZINE EC50 = 0.4467 nM 9.35
CHEMBL4526364 — EC50 = 0.6457 nM 9.19
CHEMBL4526364 — EC50 = 0.7 nM 9.15
CHEMBL240773 QUINPIROLE EC50 = 1.8 nM 8.74
CHEMBL240773 QUINPIROLE EC50 = 1.82 nM 8.74
CHEMBL4467173 — EC50 = 2.63 nM 8.58
CHEMBL4457507 — EC50 = 2.818 nM 8.55
CHEMBL3085826 — EC50 = 3.0 nM 8.52
CHEMBL4457507 — EC50 = 3.0 nM 8.52
CHEMBL4467173 — EC50 = 3.0 nM 8.52
CHEMBL3085826 — EC50 = 3.236 nM 8.49
CHEMBL4517517 — EC50 = 5.0 nM 8.30
CHEMBL4517517 — EC50 = 5.495 nM 8.26
CHEMBL4470060 — EC50 = 6.761 nM 8.17
CHEMBL4470060 — EC50 = 7.0 nM 8.15
CHEMBL4437205 — EC50 = 7.586 nM 8.12
CHEMBL4437205 — EC50 = 8.0 nM 8.10
CHEMBL4446533 — EC50 = 7.943 nM 8.10
CHEMBL4446533 — EC50 = 8.0 nM 8.10
CHEMBL4441636 — EC50 = 9.772 nM 8.01
CHEMBL4441636 — EC50 = 10.0 nM 8.00
CHEMBL4451797 — EC50 = 10.72 nM 7.97
CHEMBL4451797 — EC50 = 11.0 nM 7.96
CHEMBL3085802 — EC50 = 12.0 nM 7.92
CHEMBL3085802 — EC50 = 12.02 nM 7.92
CHEMBL3085821 — EC50 = 14.0 nM 7.85
CHEMBL4447058 — EC50 = 14.0 nM 7.85
CHEMBL3085821 — EC50 = 14.45 nM 7.84
CHEMBL4447058 — EC50 = 14.45 nM 7.84
CHEMBL4460025 — EC50 = 19.0 nM 7.72
CHEMBL4460025 — EC50 = 19.5 nM 7.71
CHEMBL4532767 — EC50 = 27.0 nM 7.57
CHEMBL4532767 — EC50 = 26.92 nM 7.57
CHEMBL3088209 — EC50 = 33.11 nM 7.48
CHEMBL3088209 — EC50 = 33.0 nM 7.48
CHEMBL4465281 — EC50 = 46.77 nM 7.33
CHEMBL4465281 — EC50 = 47.0 nM 7.33
CHEMBL3088210 — EC50 = 54.0 nM 7.27
CHEMBL3088210 — EC50 = 54.95 nM 7.26
CHEMBL4590026 — EC50 = 67.0 nM 7.17
CHEMBL4590026 — EC50 = 67.61 nM 7.17
CHEMBL4587909 — EC50 = 71.0 nM 7.15
CHEMBL4587909 — EC50 = 70.79 nM 7.15
CHEMBL3088212 — EC50 = 74.13 nM 7.13
CHEMBL3088212 — EC50 = 74.0 nM 7.13
CHEMBL4448960 — EC50 = 85.11 nM 7.07
CHEMBL4448960 — EC50 = 86.0 nM 7.07
CHEMBL4473178 — EC50 = 129.0 nM 6.89
CHEMBL4473178 — EC50 = 128.82 nM 6.89