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Assay Detail

CHEMBL5324908

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

Binding
Displacement of [3H]N-methylspiperone from human D2 receptor stably expressed in HEK293 cell membrane assessed as inhibition constant incubated for 1 hr by MicroBeta scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
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
Ki 17 5.62 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2037521 1 6.90
CHEMBL5436702 1 6.39
CHEMBL5399720 1 6.37
CHEMBL5403504 1 6.29
CHEMBL5406300 1 6.17
CHEMBL5426481 1 6.08
CHEMBL5425920 1 5.98
CHEMBL5437265 1 5.80
CHEMBL5403986 1 5.62
CHEMBL5400876 1 5.53
CHEMBL3289656 1 5.20
CHEMBL5422150 1 5.19
CHEMBL5399689 1 5.16
CHEMBL5394387 1 4.88
CHEMBL5400983 1 4.85
CHEMBL5434856 1 4.76
CHEMBL5403610 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2037521 Ki = 127.0 nM 6.90
CHEMBL5436702 Ki = 408.0 nM 6.39
CHEMBL5399720 Ki = 427.0 nM 6.37
CHEMBL5403504 Ki = 519.0 nM 6.29
CHEMBL5406300 Ki = 669.0 nM 6.17
CHEMBL5426481 Ki = 830.0 nM 6.08
CHEMBL5425920 Ki = 1050.0 nM 5.98
CHEMBL5437265 Ki = 1580.0 nM 5.80
CHEMBL5403986 Ki = 2420.0 nM 5.62
CHEMBL5400876 Ki = 2930.0 nM 5.53
CHEMBL3289656 Ki = 6370.0 nM 5.20
CHEMBL5422150 Ki = 6500.0 nM 5.19
CHEMBL5399689 Ki = 6890.0 nM 5.16
CHEMBL5394387 Ki = 13300.0 nM 4.88
CHEMBL5400983 Ki = 14000.0 nM 4.85
CHEMBL5434856 Ki = 17400.0 nM 4.76
CHEMBL5403610 Ki = 49800.0 nM 4.30