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Assay Detail

CHEMBL5534951

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

Binding
Inhibition of epibatidine-induced receptor activation at rat alpha3beta4 nAChR expressed in HEK293 cells assessed as reduction in calcium flux preincubated for 10 mins followed by epibatidine addition by FLIPR assay
ChEMBL ↗
45
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.
Rusali LE, Lopez-Hernandez AM, Kremiller KM, Kulkarni GC, Gour A, Straub CJ, Argade MD, Peters CJ, Sharma A, Toll L, Cippitelli A, Riley AP.
J Med Chem (2024) 67 : 529 -542
PubMed 38151460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.73 6.50
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5572105 — — 2 6.50
CHEMBL5590014 — — 2 6.41
CHEMBL5570620 — — 2 6.40
CHEMBL5595517 — — 2 6.40
CHEMBL5575320 — — 2 6.20
CHEMBL5542742 — — 2 6.16
CHEMBL5572459 — — 2 6.04
CHEMBL5574911 — — 2 6.01
CHEMBL5570777 — — 2 5.96
CHEMBL5567592 — — 2 5.96
CHEMBL5573348 — — 2 5.80
CHEMBL5571845 — — 2 5.80
CHEMBL5567123 — — 2 5.60
CHEMBL5572495 — — 2 5.60
CHEMBL5571457 — — 2 5.60
CHEMBL5569258 — — 2 5.50
CHEMBL5564161 — — 2 5.42
CHEMBL5565080 — — 2 5.40
CHEMBL5565186 — — 2 5.40
CHEMBL5590924 — — 2 5.20
CHEMBL5572822 — — 2 4.60
CHEMBL5542426 — — 2 4.42
CHEMBL5574217 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5572105 — IC50 = 316.23 nM 6.50
CHEMBL5572105 — IC50 = 340.0 nM 6.47
CHEMBL5590014 — IC50 = 390.0 nM 6.41
CHEMBL5595517 — IC50 = 398.11 nM 6.40
CHEMBL5570620 — IC50 = 398.11 nM 6.40
CHEMBL5590014 — IC50 = 398.11 nM 6.40
CHEMBL5595517 — IC50 = 430.0 nM 6.37
CHEMBL5570620 — IC50 = 440.0 nM 6.36
CHEMBL5575320 — IC50 = 630.96 nM 6.20
CHEMBL5575320 — IC50 = 640.0 nM 6.19
CHEMBL5542742 — IC50 = 700.0 nM 6.16
CHEMBL5542742 — IC50 = 794.33 nM 6.10
CHEMBL5572459 — IC50 = 920.0 nM 6.04
CHEMBL5574911 — IC50 = 980.0 nM 6.01
CHEMBL5574911 — IC50 = 1000.0 nM 6.00
CHEMBL5572459 — IC50 = 1000.0 nM 6.00
CHEMBL5567592 — IC50 = 1100.0 nM 5.96
CHEMBL5570777 — IC50 = 1100.0 nM 5.96
CHEMBL5570777 — IC50 = 1258.93 nM 5.90
CHEMBL5567592 — IC50 = 1258.93 nM 5.90
CHEMBL5573348 — IC50 = 1600.0 nM 5.80
CHEMBL5573348 — IC50 = 1584.89 nM 5.80
CHEMBL5571845 — IC50 = 1584.89 nM 5.80
CHEMBL5571845 — IC50 = 1700.0 nM 5.77
CHEMBL5571457 — IC50 = 2511.89 nM 5.60
CHEMBL5572495 — IC50 = 2511.89 nM 5.60
CHEMBL5567123 — IC50 = 2511.89 nM 5.60
CHEMBL5572495 — IC50 = 2600.0 nM 5.58
CHEMBL5571457 — IC50 = 2800.0 nM 5.55
CHEMBL5567123 — IC50 = 2800.0 nM 5.55
CHEMBL5569258 — IC50 = 3162.28 nM 5.50
CHEMBL5569258 — IC50 = 3400.0 nM 5.47
CHEMBL5564161 — IC50 = 3800.0 nM 5.42
CHEMBL5565080 — IC50 = 3981.07 nM 5.40
CHEMBL5564161 — IC50 = 3981.07 nM 5.40
CHEMBL5565186 — IC50 = 3981.07 nM 5.40
CHEMBL5565080 — IC50 = 4100.0 nM 5.39
CHEMBL5565186 — IC50 = 4400.0 nM 5.36
CHEMBL5590924 — IC50 = 6309.57 nM 5.20
CHEMBL5590924 — IC50 = 6900.0 nM 5.16
CHEMBL5572822 — IC50 = 25118.86 nM 4.60
CHEMBL5572822 — IC50 = 26000.0 nM 4.58
CHEMBL5542426 — IC50 = 38000.0 nM 4.42
CHEMBL5542426 — IC50 = 39810.72 nM 4.40
CHEMBL5574217 — Inhibition - % -