Table 4SAR of R1 Analogs

Compound Information: R1 AnalogsLRH1 %INH (AID 485348)LRH1 Dose Response (AID 488782)SF1 Fold Change (AID 488779)SF1 Dose Response (AID 488780)VP16 Fold Change (AID 488775)
Sample IDStructureSourceMLS IDSIDCIDLRH-1 AVG %Inhibition (at 5 μM)SDLRH-1 IC50SDSF-1 Avg Fold Change (at 5 μM)SDSF-1 IC50SDVP-16 Avg Fold Change (at 5μM)SD
SR-03000001170-1
Image ml180fu17.jpg
S896497334482521535.33% (Active)0.045921nM (Active)0.0699.33% (Inactive)0.089.2μM (Inactive)0.060%0.000
SR-03000001307-1
Image ml180fu18.jpg
P92092833148404945% (Active)0.026538nM (Active)0.065−3%0.06N/D−7%0.058
SR-03000001310-1
Image ml180fu19.jpg
SMLS003153123920928444510045542% (Active)0.147430nM (Active)0.1003.3% (Inactive)0.08N/D−5%0.050
SR-01000140561-3
Image ml180fu20.jpg
P89650166324482532% (Active)0.0872.6μM (Active)0.087−3%0.06N/D−16%0.124
SR-03000001171-1
Image ml180fu21.jpg
S896497344482521642% (Active)0.0534.8μM (Active)0.0380.67% (Inactive)0.11N/D−27%0.058
SR-03000001174-1
Image ml180fu22.jpg
SMLS003153125896497374482522334.667% (Active)0.0424.0μM (Active)0.24211.33% (Inactive)0.04N/D7% (Inactive)0.026
SR-03000001302-1
Image ml180fu23.jpg
S920928254510043332.33% (Active)0.045ND7% (Inactive)0.07ND17% (Active)0.044
SR-01000621845-2
Image ml180fu24.jpg
P8965016432406441.33% (Inactive)0.121ND−2%0.11ND−9%0.017
SR-03000001172-1
Image ml180fu25.jpg
S896497354482523036% (Active)0.03620μM (Inactive)0.017−7%0.08N/D−8%0.076
SR-03000001173-1
Image ml180fu26.jpg
S896497364482524030.33% (Active)0.07480μM (Inactive)0.027−4%0.05N/D−4%0.066
SR-01000140537-3
Image ml180fu27.jpg
P92092838324182618% (Inactive)0.156ND6%0.11ND−12%0.072
SR-03000001383-1
Image ml180fu28.jpg
S933752974538228016.33% (Inactive)0.035ND−12%0.12ND0%0.006
SR-03000001384-1
Image ml180fu29.jpg
S933752984538227538.333% (Active)0.04013μM (Inactive)0.015−4%0.13N/DN/D−6%0.085
SR-03000001385-1
Image ml180fu30.jpg
S933752994538228216% (Inactive)0.095ND5% (Inactive)0.09ND14.3% (Active)0.021
SR-03000001386-1
Image ml180fu31.jpg
S933753004538227636.67% (Active)0.091ND−112%0.19NDND
SR-03000001387-1
Image ml180fu32.jpg
S933753014538226820.3% (Inactive)0.091ND−83%0.44ND−12%0.030
SR-03000001388-1
Image ml180fu33.jpg
S933753024538228516% (Inactive)0.090ND13.33% (Inactive)0.10ND16% (Active)0.090
SR-03000001389-1
Image ml180fu34.jpg
S933753034538228320% (Inactive)0.046ND−9%0.07ND1.3% (Inactive)0.012
SR-01000140541-4
Image ml180fu35.jpg
P9209284135717345.33% (Inactive)0.055ND4.33% (Inactive)0.06ND0%0.100
SR-03000001175-1
Image ml180fu36.jpg
S89649738448252170% (Inactive)0.121ND1% (Inactive)0.06ND−5%0.084
SR-03000001176-1
Image ml180fu37.jpg
S89649739448252192.67% (Inactive)0.081ND−14%0.17ND−4%0.105
SR-03000001300-1
Image ml180fu38.jpg
S9209282345100453−0.30%0.173ND−13%0.21ND−48%0.157
SR-03000001301-1
Image ml180fu39.jpg
S920928244510046216.67% (Inactive)0.055ND23.67% (Active)0.08ND−5%0.031
SR-01000607332-2
Image ml180fu40.jpg
S92092826323717211% (Inactive)0.046ND6% (Inactive)0.05ND16.67% (Active)0.235
SR-03000001390-1
Image ml180fu41.jpg
S93375304453822693.33% (Inactive)0.042ND−49%0.01ND26% (Active)0.020
SR-03000001391-1
Image ml180fu42.jpg
S933753054538227211%0.144ND5.33% (Inactive)0.13ND13.3% (Active)0.050
SR-03000001403-1
Image ml180fu43.jpg
S935779164548013516% (Inactive)0.050ND−19%0.06ND1.3% (Inactive)0.257
SR-03000001404-1
Image ml180fu44.jpg
S935779174548013317% (Inactive)0.053ND−23%0.06ND−4%0.035
SR-03000001410-1
Image ml180fu45.jpg
S93577923454801393.333% (Inactive)0.035ND9% (Inactive)0.04ND2.67% (Inactive)0.032
SR-01000140539-2
Image ml180fu46.jpg
P8578676214792441.667% (Inactive)0.012ND4.67% (Inactive)0.02ND1.33% (Inactive)0.015
SR-03000001303-1
Image ml180fu47.jpg
S920928274510046013.33% (Inactive)0.115ND8.67% (Inactive)0.10ND26% (Active)0.131
SR-03000001304-1
Image ml180fu48.jpg
S92092828451004304% (Inactive)0.139ND−8%0.03ND11.33% (Inactive)0.045
SR-03000001305-1
Image ml180fu49.jpg
S92092829451004390%0.006ND1.67% (Inactive)0.08ND8% (Inactive)0.072
SR-01000621846-2
Image ml180fu50.jpg
P9209283932390852.33% (Inactive)0.045ND9% (Inactive)0.05ND26.3% (Active)0.110
SR-01000140511-3
Image ml180fu51.jpg
P92092840324552216% (Inactive)0.183ND19.3% (Inactive)0.14ND−6%0.053
SR-01000140541-4
Image ml180fu52.jpg
P9209284135717345.33% (Inactive)0.061ND5.3% (Inactive)0.08ND0%0.100
SR-01000101040-3
Image ml180fu53.jpg
P92092842357173510% (Inactive)0.020ND−5%0.07ND5.67% (Inactive)0.060
SR-01000140507-3
Image ml180fu54.jpg
S92092831414105820.33% (Inactive)0.101ND23% (Inactive)0.13ND0%0.006
SR-03000001306-1
Image ml180fu55.jpg
S92092830451004328.67% (Inactive)0.075ND5% (Inactive)0.17ND−6%0.053
SR-01000101020-3
Image ml180fu56.jpg
S9209283232426885.33% (Inactive)0.136ND0%0.01ND9% (Inactive)0.052
SR-03000001311-1
Image ml180fu57.jpg
S920928454510043814.33% (Inactive)0.127ND23%0.08ND−11%0.032

ND indicates a compound was not tested in the indicated assay due to lack of LRH1 activity compared to probe in the 3X%INH assay

From: Discovery of Inverse Agonists for the Liver Receptor Homologue-1 (LRH1; NR5A2)

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.