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Assay Detail

CHEMBL915382

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Binding
Activity at human alpha-2GlyR expressed in HEK293 cells by FMP assay
ChEMBL ↗
45
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glycine receptor subunit alpha-2 (CHEMBL5871) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Jensen AA, Begum N, Vogensen SB, Knapp KM, Gundertofte K, Dzyuba SV, Ishii H, Nakanishi K, Kristiansen U, Strømgaard K.
J Med Chem (2007) 50 : 1610 -1617
PubMed 17352465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.16 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113267 GINKGOLIDE M — 2 5.90
CHEMBL465161 GINKGOLIDE A — 2 5.70
CHEMBL514432 GINKOLIDE B — 2 5.43
CHEMBL426556 — — 2 5.34
CHEMBL221823 — — 2 5.11
CHEMBL221821 GINKGOLIDE C — 2 5.10
CHEMBL373969 3,14-DIDEHYDROGINKGOLIDE A — 2 5.02
CHEMBL388075 — — 2 4.92
CHEMBL374004 GINKGOLIDE J — 2 4.92
CHEMBL221715 — — 2 4.90
CHEMBL376289 — — 2 4.54
CHEMBL373832 — — 1 -
CHEMBL375821 — — 1 -
CHEMBL374058 — — 1 -
CHEMBL222345 — — 1 -
CHEMBL223761 — — 1 -
CHEMBL224937 — — 1 -
CHEMBL376777 — — 1 -
CHEMBL225471 — — 1 -
CHEMBL221355 — — 1 -
CHEMBL222405 — — 1 -
CHEMBL221937 — — 1 -
CHEMBL221769 — — 1 -
CHEMBL374102 — — 1 -
CHEMBL223081 — — 1 -
CHEMBL412540 — — 1 -
CHEMBL225470 10-METHOXYMETHYLOXY-GINKGOLIDE A — 1 -
CHEMBL412384 — — 1 -
CHEMBL222222 10-ACETOXY-GINKGOLIDE B — 1 -
CHEMBL376302 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113267 GINKGOLIDE M IC50 = 1258.93 nM 5.90
CHEMBL2113267 GINKGOLIDE M IC50 = 1300.0 nM 5.89
CHEMBL465161 GINKGOLIDE A IC50 = 1995.26 nM 5.70
CHEMBL465161 GINKGOLIDE A IC50 = 2100.0 nM 5.68
CHEMBL514432 GINKOLIDE B IC50 = 3700.0 nM 5.43
CHEMBL514432 GINKOLIDE B IC50 = 3981.07 nM 5.40
CHEMBL426556 — IC50 = 4600.0 nM 5.34
CHEMBL426556 — IC50 = 5011.87 nM 5.30
CHEMBL221823 — IC50 = 7800.0 nM 5.11
CHEMBL221823 — IC50 = 7943.28 nM 5.10
CHEMBL221821 GINKGOLIDE C IC50 = 7943.28 nM 5.10
CHEMBL221821 GINKGOLIDE C IC50 = 8200.0 nM 5.09
CHEMBL373969 3,14-DIDEHYDROGINKGOLIDE A IC50 = 9500.0 nM 5.02
CHEMBL373969 3,14-DIDEHYDROGINKGOLIDE A IC50 = 10000.0 nM 5.00
CHEMBL388075 — IC50 = 12000.0 nM 4.92
CHEMBL374004 GINKGOLIDE J IC50 = 12000.0 nM 4.92
CHEMBL374004 GINKGOLIDE J IC50 = 12589.25 nM 4.90
CHEMBL221715 — IC50 = 12589.25 nM 4.90
CHEMBL388075 — IC50 = 12589.25 nM 4.90
CHEMBL221715 — IC50 = 13000.0 nM 4.89
CHEMBL376289 — IC50 = 29000.0 nM 4.54
CHEMBL376289 — IC50 = 31622.78 nM 4.50
CHEMBL373436 — IC50 > 100000.0 nM -
CHEMBL385320 — IC50 > 100000.0 nM -
CHEMBL222534 — IC50 > 100000.0 nM -
CHEMBL387106 — IC50 > 100000.0 nM -
CHEMBL373832 — IC50 > 100000.0 nM -
CHEMBL375821 — IC50 > 100000.0 nM -
CHEMBL374058 — IC50 > 100000.0 nM -
CHEMBL222345 — IC50 > 100000.0 nM -
CHEMBL223761 — IC50 > 100000.0 nM -
CHEMBL224937 — IC50 > 100000.0 nM -
CHEMBL376777 — IC50 > 100000.0 nM -
CHEMBL225471 — IC50 > 100000.0 nM -
CHEMBL221355 — IC50 > 100000.0 nM -
CHEMBL222405 — IC50 > 100000.0 nM -
CHEMBL221937 — IC50 > 100000.0 nM -
CHEMBL221769 — IC50 > 100000.0 nM -
CHEMBL374102 — IC50 > 100000.0 nM -
CHEMBL223081 — IC50 > 100000.0 nM -
CHEMBL412540 — IC50 > 100000.0 nM -
CHEMBL225470 10-METHOXYMETHYLOXY-GINKGOLIDE A IC50 > 100000.0 nM -
CHEMBL412384 — IC50 > 100000.0 nM -
CHEMBL222222 10-ACETOXY-GINKGOLIDE B IC50 > 100000.0 nM -
CHEMBL376302 — IC50 > 100000.0 nM -