TRPML3/2 Agonist SAR Table 1Secondary Arylsulfonamides Scaffold

Compound InformationHTS InformationProbe Development Information
CompoundStructureCIDSIDMLSVendorVendor Catalog IDTRPML3 Dose Response (AID 1562) EC50, μMTRPN1 Dose Response Counterscreen (AID 1682) EC50, μMSIDTRPML3 Dose Response EC50, μM (AID 2116)TRPN1 Dose Response EC50, μM (AID 2116)TRPML3 Patch Clamp Assay (AID 2116)TRPN1 Patch Clamp Assay (AID 2116)TRPML3, TRPML2 Fura-2 Imaging (AID 2116)Fura-2 Profiling Assays (AID 2116)
Probe
Image ml123fu18.jpg
291164624801657MLS 000713637AsinexBAS 03787124Active (0.873)Inactive (>29.9)85786753Active (0.451)Inactive (14.0)ActiveInactiveActiveInactive in hTRPML1, hTRPM2, mTRPV2, hTRPC3, drTRPN1, and hTRPA1.
Analog 1
Image ml123fu19.jpg
211103714746905MLS 000570381 MLSEnamineT5241132Active (0.872)Inactive (>29.9)85786755Active (0.624)Inactive (>29.9)ActiveInactiveInactiveInactive in hTRPML1, hTRPM2, mTRPV2, hTRPC3, drTRPN1, and hTRPA1. Inactive in hTRPML1,
Analog 2
Image ml123fu20.jpg
21249083716245000054019 MLSEnamineT5252809Active (1.36)Inactive (>29.9)85786754Active (1.09)Inactive (>29.9)ActiveInactiveInactivehTRPM2, mTRPV2, hTRPC3, drTRPN1, and hTRPA1. Inactive in hTRPML1,
Analog 3
Image ml123fu21.jpg
81864717414375000575428Chem Bridge5182458Active (1.59)Inactive (>29.9)85786756Active (2.14)Inactive (>29.9)ActiveInactiveInactivehTRPM2, mTRPV2, hTRPC3, drTRPN1, and hTRPA1.
Analog 4
Image ml123fu22.jpg
281404026731263MLS 000850372MaybridgeHTS 08158Active (2.3)Inactive (>29.9)Not tested due to lower target potency in AID 1562, compared to the probe.
Analog 5
Image ml123fu23.jpg
207825522405272MLS 000394056EnamineT5268454Active (2.48)Inactive (>29.9)

From: Campaign to Identify Agonists of Transient Receptor Potential Channels 3 and 2 (TRPML3 & TRPML2)

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

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