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Assay Detail

CHEMBL803935

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Binding
Tested in vitro for the concentration required to inhibit specific [3H]DTG radioligand binding to sigma receptor on guinea pig brain membrane
ChEMBL ↗
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist.
Reddy NL, Hu LY, Cotter RE, Fischer JB, Wong WJ, McBurney RN, Weber E, Holmes DL, Wong ST, Prasad R.
J Med Chem (1994) 37 : 260 -267
PubMed 8295213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 6.28 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL78777 — — 1 8.10
CHEMBL312600 — — 1 7.89
CHEMBL310170 — — 1 7.85
CHEMBL315051 — — 1 7.54
CHEMBL282433 DITOLYLGUANIDINE — 1 7.51
CHEMBL81070 — — 1 7.48
CHEMBL90508 — — 1 7.40
CHEMBL79437 — — 1 7.38
CHEMBL309603 — — 1 7.37
CHEMBL91713 — — 1 7.27
CHEMBL78306 — — 1 7.23
CHEMBL88660 — — 1 7.22
CHEMBL88932 — — 1 7.12
CHEMBL91628 — — 1 7.09
CHEMBL280243 — — 1 7.06
CHEMBL89344 — — 1 7.04
CHEMBL91791 — — 1 7.04
CHEMBL82078 — — 1 7.02
CHEMBL81678 — — 1 6.90
CHEMBL90975 — — 1 6.85
CHEMBL79509 — — 1 6.78
CHEMBL430455 — — 1 6.62
CHEMBL81626 — — 1 6.62
CHEMBL78083 — — 1 6.61
CHEMBL330551 — — 1 6.61
CHEMBL314423 — — 1 6.47
CHEMBL91222 — — 1 6.46
CHEMBL431214 — — 1 6.46
CHEMBL78411 — — 1 6.45
CHEMBL77675 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL78777 — IC50 = 8.0 nM 8.10
CHEMBL312600 — IC50 = 13.0 nM 7.89
CHEMBL310170 — IC50 = 14.0 nM 7.85
CHEMBL315051 — IC50 = 29.0 nM 7.54
CHEMBL282433 DITOLYLGUANIDINE IC50 = 31.0 nM 7.51
CHEMBL81070 — IC50 = 33.0 nM 7.48
CHEMBL90508 — IC50 = 40.0 nM 7.40
CHEMBL79437 — IC50 = 42.0 nM 7.38
CHEMBL309603 — IC50 = 43.0 nM 7.37
CHEMBL91713 — IC50 = 54.0 nM 7.27
CHEMBL78306 — IC50 = 59.0 nM 7.23
CHEMBL88660 — IC50 = 60.0 nM 7.22
CHEMBL88932 — IC50 = 75.0 nM 7.12
CHEMBL91628 — IC50 = 82.0 nM 7.09
CHEMBL280243 — IC50 = 88.0 nM 7.06
CHEMBL89344 — IC50 = 91.0 nM 7.04
CHEMBL91791 — IC50 = 92.0 nM 7.04
CHEMBL82078 — IC50 = 96.0 nM 7.02
CHEMBL81678 — IC50 = 125.0 nM 6.90
CHEMBL90975 — IC50 = 140.0 nM 6.85
CHEMBL79509 — IC50 = 165.0 nM 6.78
CHEMBL430455 — IC50 = 240.0 nM 6.62
CHEMBL81626 — IC50 = 242.0 nM 6.62
CHEMBL78083 — IC50 = 245.0 nM 6.61
CHEMBL330551 — IC50 = 247.0 nM 6.61
CHEMBL314423 — IC50 = 341.0 nM 6.47
CHEMBL431214 — IC50 = 343.0 nM 6.46
CHEMBL91222 — IC50 = 351.0 nM 6.46
CHEMBL78411 — IC50 = 356.0 nM 6.45
CHEMBL77675 — IC50 = 397.0 nM 6.40
CHEMBL81602 — IC50 = 535.0 nM 6.27
CHEMBL328986 — IC50 = 1000.0 nM 6.00
CHEMBL91145 — IC50 = 1070.0 nM 5.97
CHEMBL89811 — IC50 = 1210.0 nM 5.92
CHEMBL329623 — IC50 = 1370.0 nM 5.86
CHEMBL314710 — IC50 = 1410.0 nM 5.85
CHEMBL420979 — IC50 = 1860.0 nM 5.73
CHEMBL310729 — IC50 = 1990.0 nM 5.70
CHEMBL92095 — IC50 = 2100.0 nM 5.68
CHEMBL420245 — IC50 = 2190.0 nM 5.66
CHEMBL88146 — IC50 = 2290.0 nM 5.64
CHEMBL92484 APTIGANEL IC50 = 2540.0 nM 5.59
CHEMBL265549 — IC50 = 2640.0 nM 5.58
CHEMBL91946 — IC50 = 2700.0 nM 5.57
CHEMBL431462 — IC50 = 2740.0 nM 5.56
CHEMBL90643 — IC50 = 2900.0 nM 5.54
CHEMBL90326 — IC50 = 3020.0 nM 5.52
CHEMBL88465 — IC50 = 4800.0 nM 5.32
CHEMBL90809 — IC50 = 6130.0 nM 5.21
CHEMBL412674 — IC50 = 6280.0 nM 5.20