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Assay Detail

CHEMBL5359162

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

Functional
Partial agonist activity at human 5-HT2CR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL ↗
38
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-T-REx-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Spiro[chromene-2,4'-piperidine]s as Potent, Selective, and G<sub>q</sub>-Biased 5-HT<sub>2C</sub> Receptor Partial Agonists.
Jiang G, Zhang B, Zhang X, Chen F, Qin W, Chen JL, Tian S, Shui W, Ye N.
ACS Med Chem Lett (2024) 15 : 99 -106
PubMed 38229745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 6.34 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 9.92
CHEMBL5417234 — — 2 7.00
CHEMBL5399965 — — 2 6.92
CHEMBL4913232 — — 2 6.83
CHEMBL5396618 — — 2 6.82
CHEMBL5430054 — — 2 6.80
CHEMBL5414076 — — 2 6.67
CHEMBL5409492 — — 2 6.50
CHEMBL5409777 — — 4 6.32
CHEMBL5414815 — — 2 6.31
CHEMBL5428578 — — 2 6.10
CHEMBL5395596 — — 2 6.02
CHEMBL5424008 — — 2 5.70
CHEMBL5421733 — — 2 5.70
CHEMBL5406797 — — 2 5.51
CHEMBL5407824 — — 2 5.51
CHEMBL5397301 — — 2 5.47
CHEMBL5434839 — — 2 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 0.12 nM 9.92
CHEMBL39 SEROTONIN EC50 = 0.1259 nM 9.90
CHEMBL5417234 — EC50 = 100.0 nM 7.00
CHEMBL5417234 — EC50 = 103.1 nM 6.99
CHEMBL5399965 — EC50 = 121.5 nM 6.92
CHEMBL5399965 — EC50 = 125.89 nM 6.90
CHEMBL4913232 — EC50 = 147.1 nM 6.83
CHEMBL5396618 — EC50 = 149.9 nM 6.82
CHEMBL4913232 — EC50 = 158.49 nM 6.80
CHEMBL5396618 — EC50 = 158.49 nM 6.80
CHEMBL5430054 — EC50 = 158.49 nM 6.80
CHEMBL5430054 — EC50 = 169.8 nM 6.77
CHEMBL5414076 — EC50 = 215.0 nM 6.67
CHEMBL5409492 — EC50 = 316.23 nM 6.50
CHEMBL5409492 — EC50 = 329.6 nM 6.48
CHEMBL5409777 — EC50 = 475.8 nM 6.32
CHEMBL5414815 — EC50 = 488.4 nM 6.31
CHEMBL5409777 — EC50 = 501.19 nM 6.30
CHEMBL5414815 — EC50 = 501.19 nM 6.30
CHEMBL5428578 — EC50 = 794.33 nM 6.10
CHEMBL5428578 — EC50 = 928.9 nM 6.03
CHEMBL5395596 — EC50 = 949.8 nM 6.02
CHEMBL5395596 — EC50 = 1000.0 nM 6.00
CHEMBL5421733 — EC50 = 1995.26 nM 5.70
CHEMBL5424008 — EC50 = 1995.26 nM 5.70
CHEMBL5414076 — EC50 = 1995.26 nM 5.70
CHEMBL5421733 — EC50 = 2055.0 nM 5.69
CHEMBL5424008 — EC50 = 2494.0 nM 5.60
CHEMBL5409777 — EC50 = 2511.89 nM 5.60
CHEMBL5409777 — EC50 = 2646.0 nM 5.58
CHEMBL5406797 — EC50 = 3111.0 nM 5.51
CHEMBL5407824 — EC50 = 3062.0 nM 5.51
CHEMBL5406797 — EC50 = 3162.28 nM 5.50
CHEMBL5407824 — EC50 = 3162.28 nM 5.50
CHEMBL5397301 — EC50 = 3380.0 nM 5.47
CHEMBL5434839 — EC50 = 3738.0 nM 5.43
CHEMBL5434839 — EC50 = 3981.07 nM 5.40
CHEMBL5397301 — EC50 = 3981.07 nM 5.40