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Assay Detail

CHEMBL4346404

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Functional
Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Taste receptor type 2 member 8 (CHEMBL3988599) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.
Fotsing JR, Darmohusodo V, Patron AP, Ching BW, Brady T, Arellano M, Chen Q, Davis TJ, Liu H, Servant G, Zhang L, Williams M, Saganich M, Ditschun T, Tachdjian C, Karanewsky DS.
J Med Chem (2020) 63 : 4957 -4977
PubMed 32330040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.37 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3933031 — — 1 7.70
CHEMBL4108527 — — 1 7.70
CHEMBL3961116 — — 1 7.70
CHEMBL3924866 — — 1 7.70
CHEMBL3948082 — — 1 7.40
CHEMBL3915586 — — 1 7.40
CHEMBL3970005 — — 1 7.40
CHEMBL3907822 — — 1 7.22
CHEMBL3902340 — — 1 7.00
CHEMBL3979660 — — 1 7.00
CHEMBL3964777 — — 1 7.00
CHEMBL3896824 — — 1 7.00
CHEMBL3929225 — — 1 7.00
CHEMBL3891080 — — 1 7.00
CHEMBL3965292 — — 1 7.00
CHEMBL3917282 — — 1 6.70
CHEMBL3898835 — — 1 6.70
CHEMBL3932026 — — 1 6.70
CHEMBL4514970 — — 1 6.70
CHEMBL3950626 — — 1 6.52
CHEMBL3945185 — — 1 6.52
CHEMBL3901756 — — 1 6.52
CHEMBL4452065 — — 1 6.52
CHEMBL3918801 — — 1 6.40
CHEMBL4469393 — — 1 6.40
CHEMBL3941028 — — 1 6.40
CHEMBL3891877 — — 1 6.40
CHEMBL4567380 — — 1 6.30
CHEMBL3899833 — — 1 6.30
CHEMBL3899757 — — 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3933031 — IC50 = 20.0 nM 7.70
CHEMBL3924866 — IC50 = 20.0 nM 7.70
CHEMBL3961116 — IC50 = 20.0 nM 7.70
CHEMBL4108527 — IC50 = 20.0 nM 7.70
CHEMBL3948082 — IC50 = 40.0 nM 7.40
CHEMBL3915586 — IC50 = 40.0 nM 7.40
CHEMBL3970005 — IC50 = 40.0 nM 7.40
CHEMBL3907822 — IC50 = 60.0 nM 7.22
CHEMBL3979660 — IC50 = 100.0 nM 7.00
CHEMBL3964777 — IC50 = 100.0 nM 7.00
CHEMBL3896824 — IC50 = 100.0 nM 7.00
CHEMBL3929225 — IC50 = 100.0 nM 7.00
CHEMBL3891080 — IC50 = 100.0 nM 7.00
CHEMBL3965292 — IC50 = 100.0 nM 7.00
CHEMBL3902340 — IC50 = 100.0 nM 7.00
CHEMBL3917282 — IC50 = 200.0 nM 6.70
CHEMBL4514970 — IC50 = 200.0 nM 6.70
CHEMBL3932026 — IC50 = 200.0 nM 6.70
CHEMBL3898835 — IC50 = 200.0 nM 6.70
CHEMBL3950626 — IC50 = 300.0 nM 6.52
CHEMBL3945185 — IC50 = 300.0 nM 6.52
CHEMBL3901756 — IC50 = 300.0 nM 6.52
CHEMBL4452065 — IC50 = 300.0 nM 6.52
CHEMBL3891877 — IC50 = 400.0 nM 6.40
CHEMBL3941028 — IC50 = 400.0 nM 6.40
CHEMBL3918801 — IC50 = 400.0 nM 6.40
CHEMBL4469393 — IC50 = 400.0 nM 6.40
CHEMBL4567380 — IC50 = 500.0 nM 6.30
CHEMBL3899833 — IC50 = 500.0 nM 6.30
CHEMBL3899757 — IC50 = 700.0 nM 6.16
CHEMBL3939850 — IC50 = 700.0 nM 6.16
CHEMBL4447100 — IC50 = 700.0 nM 6.16
CHEMBL3890731 — IC50 = 800.0 nM 6.10
CHEMBL4456506 — IC50 = 800.0 nM 6.10
CHEMBL3908324 — IC50 = 800.0 nM 6.10
CHEMBL3930312 — IC50 = 900.0 nM 6.05
CHEMBL3912134 — IC50 = 1000.0 nM 6.00
CHEMBL4526144 — IC50 = 1000.0 nM 6.00
CHEMBL3921262 — IC50 = 1000.0 nM 6.00
CHEMBL4530528 — IC50 = 1000.0 nM 6.00
CHEMBL4588973 — IC50 = 1000.0 nM 6.00
CHEMBL3910649 — IC50 = 1000.0 nM 6.00
CHEMBL3916540 — IC50 = 1100.0 nM 5.96
CHEMBL4579065 — IC50 = 1100.0 nM 5.96
CHEMBL3927851 — IC50 = 1700.0 nM 5.77
CHEMBL3908801 — IC50 = 1900.0 nM 5.72
CHEMBL3933783 — IC50 = 2000.0 nM 5.70
CHEMBL4471870 — IC50 = 2000.0 nM 5.70
CHEMBL4443466 — IC50 = 2000.0 nM 5.70
CHEMBL4448191 — IC50 = 2300.0 nM 5.64