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Assay Detail

CHEMBL5324914

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Functional
Agonist activity at human D4 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Boateng CA, Nilson AN, Placide R, Pham ML, Jakobs FM, Boldizsar N, McIntosh S, Stallings LS, Korankyi IV, Kelshikar S, Shah N, Panasis D, Muccilli A, Ladik M, Maslonka B, McBride C, Sanchez MX, Akca E, Alkhatib M, Saez J, Nguyen C, Kurtyan E, DePierro J, Crowthers R, Brunt D, Bonifazi A, Newman AH, Rais R, Slusher BS, Free RB, Sibley DR, Stewart KD, Wu C, Hemby SE, Keck TM.
J Med Chem (2023) 66 : 12141 -12162
PubMed 37646374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 7.62 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59 DOPAMINE 4.0 1 8.42
CHEMBL3289656 1 8.36
CHEMBL5400876 1 7.97
CHEMBL5406300 1 7.90
CHEMBL5403610 1 7.53
CHEMBL5399720 1 7.41
CHEMBL5399689 1 6.82
CHEMBL5403986 1 6.57
CHEMBL5436702 1 -
CHEMBL5425920 1 -
CHEMBL5426481 1 -
CHEMBL5437265 1 -
CHEMBL5434856 1 -
CHEMBL5394387 1 -
CHEMBL5422150 1 -
CHEMBL5400983 1 -
CHEMBL2037521 1 -
CHEMBL5403504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59 DOPAMINE EC50 = 3.78 nM 8.42
CHEMBL3289656 EC50 = 4.34 nM 8.36
CHEMBL5400876 EC50 = 10.6 nM 7.97
CHEMBL5406300 EC50 = 12.7 nM 7.90
CHEMBL5403610 EC50 = 29.5 nM 7.53
CHEMBL5399720 EC50 = 38.6 nM 7.41
CHEMBL5399689 EC50 = 150.0 nM 6.82
CHEMBL5403986 EC50 = 272.0 nM 6.57
CHEMBL5436702 EC50 - -
CHEMBL5425920 EC50 - -
CHEMBL5426481 EC50 - -
CHEMBL5437265 EC50 - -
CHEMBL5434856 EC50 - -
CHEMBL5394387 EC50 - -
CHEMBL5422150 EC50 - -
CHEMBL5400983 EC50 - -
CHEMBL2037521 EC50 - -
CHEMBL5403504 EC50 - -