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Assay Detail

CHEMBL4820882

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

Binding
Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay
ChEMBL ↗
54
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type tsA201
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glycine receptor (alpha-1/beta) (CHEMBL2363052) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

C-2-Linked Dimeric Strychnine Analogues as Bivalent Ligands Targeting Glycine Receptors.
Zlotos DP, Abdelmalek CM, Botros LS, Banoub MM, Mandour YM, Breitinger U, El Nady A, Breitinger HG, Sotriffer C, Villmann C, Jensen AA, Holzgrabe U.
J Nat Prod (2021) 84 : 382 -394
PubMed 33596384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.46 6.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4865584 — — 2 6.69
CHEMBL227934 STRYCHNINE -1.0 2 6.29
CHEMBL4849489 — — 2 6.29
CHEMBL4870655 — — 2 6.17
CHEMBL4870669 — — 2 6.06
CHEMBL4848356 — — 2 5.77
CHEMBL4865147 — — 2 5.75
CHEMBL4850957 — — 2 5.75
CHEMBL4870499 — — 2 5.72
CHEMBL4864670 — — 2 5.70
CHEMBL4867244 — — 2 5.66
CHEMBL4857611 — — 2 5.66
CHEMBL4851242 — — 2 5.62
CHEMBL4855686 — — 2 5.41
CHEMBL4856988 — — 2 5.39
CHEMBL4849579 — — 2 5.24
CHEMBL4865348 — — 2 5.00
CHEMBL4871973 — — 2 5.00
CHEMBL4873527 — — 2 5.00
CHEMBL4864603 — — 2 5.00
CHEMBL4849060 — — 2 5.00
CHEMBL4860026 — — 2 5.00
CHEMBL4873219 — — 2 4.70
CHEMBL4873023 — — 2 4.52
CHEMBL4878671 — — 2 4.50
CHEMBL4863367 — — 2 -
CHEMBL4861263 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4865584 — IC50 = 204.17 nM 6.69
CHEMBL4865584 — IC50 = 210.0 nM 6.68
CHEMBL227934 STRYCHNINE IC50 = 510.0 nM 6.29
CHEMBL4849489 — IC50 = 512.86 nM 6.29
CHEMBL4849489 — IC50 = 510.0 nM 6.29
CHEMBL227934 STRYCHNINE IC50 = 512.86 nM 6.29
CHEMBL4870655 — IC50 = 680.0 nM 6.17
CHEMBL4870655 — IC50 = 676.08 nM 6.17
CHEMBL4870669 — IC50 = 870.96 nM 6.06
CHEMBL4870669 — IC50 = 880.0 nM 6.06
CHEMBL4848356 — IC50 = 1700.0 nM 5.77
CHEMBL4848356 — IC50 = 1737.8 nM 5.76
CHEMBL4865147 — IC50 = 1800.0 nM 5.75
CHEMBL4850957 — IC50 = 1778.28 nM 5.75
CHEMBL4850957 — IC50 = 1800.0 nM 5.75
CHEMBL4865147 — IC50 = 1778.28 nM 5.75
CHEMBL4870499 — IC50 = 1900.0 nM 5.72
CHEMBL4870499 — IC50 = 1949.84 nM 5.71
CHEMBL4864670 — IC50 = 2000.0 nM 5.70
CHEMBL4864670 — IC50 = 1995.26 nM 5.70
CHEMBL4857611 — IC50 = 2200.0 nM 5.66
CHEMBL4867244 — IC50 = 2200.0 nM 5.66
CHEMBL4857611 — IC50 = 2238.72 nM 5.65
CHEMBL4867244 — IC50 = 2238.72 nM 5.65
CHEMBL4851242 — IC50 = 2398.83 nM 5.62
CHEMBL4851242 — IC50 = 2400.0 nM 5.62
CHEMBL4855686 — IC50 = 3890.45 nM 5.41
CHEMBL4855686 — IC50 = 3900.0 nM 5.41
CHEMBL4856988 — IC50 = 4100.0 nM 5.39
CHEMBL4856988 — IC50 = 4073.8 nM 5.39
CHEMBL4849579 — IC50 = 5800.0 nM 5.24
CHEMBL4849579 — IC50 = 5888.44 nM 5.23
CHEMBL4864603 — IC50 = 10000.0 nM 5.00
CHEMBL4865348 — IC50 = 10000.0 nM 5.00
CHEMBL4871973 — IC50 = 10000.0 nM 5.00
CHEMBL4871973 — IC50 = 10000.0 nM 5.00
CHEMBL4873527 — IC50 = 10000.0 nM 5.00
CHEMBL4873527 — IC50 = 10000.0 nM 5.00
CHEMBL4864603 — IC50 = 10000.0 nM 5.00
CHEMBL4849060 — IC50 = 10000.0 nM 5.00
CHEMBL4849060 — IC50 = 10000.0 nM 5.00
CHEMBL4860026 — IC50 = 10000.0 nM 5.00
CHEMBL4860026 — IC50 = 10000.0 nM 5.00
CHEMBL4865348 — IC50 = 10000.0 nM 5.00
CHEMBL4873219 — IC50 = 20000.0 nM 4.70
CHEMBL4873023 — IC50 = 30000.0 nM 4.52
CHEMBL4878671 — IC50 = 31622.78 nM 4.50
CHEMBL4873023 — IC50 = 31622.78 nM 4.50
CHEMBL4878671 — IC50 = 50000.0 nM 4.30
CHEMBL4873219 — IC50 = 50118.72 nM 4.30