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mGlu5 receptor

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Target not currently curated in GtoImmuPdb

Target id: 293

Nomenclature: mGlu5 receptor

Family: Metabotropic glutamate receptors

Contents:

Gene and Protein Information Click here for help
class C G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 1212 11q14.2-q14.3 GRM5 glutamate metabotropic receptor 5 59-60
Mouse 7 1203 7 D3 Grm5 glutamate receptor, metabotropic 5
Rat 7 1203 1q32 Grm5 glutamate metabotropic receptor 5 1,40
Previous and Unofficial Names Click here for help
mGluR5 | GPRC1E | glutamate receptor
Database Links Click here for help
Specialist databases
GPCRDB grm5_human (Hs), grm5_mouse (Mm), grm5_rat (Rn)
Other databases
ChEMBL Target CHEMBL3227 (Hs), CHEMBL1641352 (Mm), CHEMBL2564 (Rn)
DrugBank Target P41594 (Hs)
Ensembl Gene ENSG00000168959 (Hs), ENSMUSG00000049583 (Mm), ENSRNOG00000016429 (Rn)
Entrez Gene 2915 (Hs), 108071 (Mm), 24418 (Rn)
Human Protein Atlas ENSG00000168959 (Hs)
KEGG Gene hsa:2915 (Hs), mmu:108071 (Mm), rno:24418 (Rn)
OMIM 604102 (Hs)
Pharos P41594 (Hs)
RefSeq Nucleotide NM_000842 (Hs), NM_001143831 (Hs), NM_001081414 (Mm), NM_017012 (Rn)
RefSeq Protein NP_001137303 (Hs), NP_000833 (Hs), NP_001074883 (Mm), NP_058708 (Rn)
UniProtKB P41594 (Hs), Q3UVX5 (Mm), P31424 (Rn)
Wikipedia GRM5 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator mavoglurant
PDB Id:  4OO9
Ligand:  mavoglurant
Resolution:  2.6Å
Species:  Human
References:  23
Natural/Endogenous Ligands Click here for help
L-glutamic acid
Comments: Other endogenous ligands include L-aspartic acid, L-serine-O-phosphate, NAAG and L-cysteine sulphinic acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0424465 Small molecule or natural product Rn Agonist 6.8 pEC50 81
⤷ pEC50 6.8 (EC50 1.71x10-7 M) [81]
VU0092273 Small molecule or natural product Rn Agonist 5.9 pEC50 64
⤷ pEC50 5.9 (EC50 1.3x10-6 M) [64]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.0 – 5.5 pEC50 71
⤷ pEC50 5.0 – 5.5 [71]
(S)-(+)-CBPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 4.3 pEC50 55
⤷ pEC50 4.3 (EC50 4.7x10-5 M) [55]
quisqualate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 pIC50 62
⤷ pIC50 7.5 [62]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.1 pIC50 62
⤷ pIC50 6.1 [62]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.8 pIC50 62
⤷ pIC50 5.8 [62]
(1S,3R)-ACPD Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.7 pIC50 62
⤷ pIC50 5.7 [62]
ibotenic acid Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.7 pIC50 62
⤷ pIC50 5.7 [62]
3,5-DHPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.4 pIC50 62
⤷ pIC50 5.4 [62]
(S)-3HPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.0 pIC50 62
⤷ pIC50 5.0 [62]
CHPG Small molecule or natural product Hs Full agonist 3.4 pIC50 62
⤷ pIC50 3.4 [62]
View species-specific agonist tables
Agonist Comments
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu5. This is the only study describing affinity values for these compounds. More information on agonist potencies determined from functional studies can be obtained from [83]. So far no differences have been reported for the agonist affinities between the rat and the human receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[11C]JNJ-16567083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 5.6 pKi 37
⤷ pKi 5.6 (Ki 2.366x10-6 M) [37]
methoxy-MPEP Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 8.4 pIC50 29
⤷ pIC50 8.4 (IC50 3.6x10-9 M) [29]
Description: [3H]-M-MPEP displacement assay.
ACDPP Small molecule or natural product Hs Antagonist 6.9 pIC50 6
⤷ pIC50 6.9 [6]
(S)-4C3HPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.6 pIC50 62
⤷ pIC50 5.6 [62]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.1 pIC50 43
⤷ pIC50 5.1 [43]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 4.7 pIC50 62
⤷ pIC50 4.7 [62]
(S)-4CPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.6 pIC50 62
⤷ pIC50 4.6 [62]
(+)-MCPG Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 3.7 pIC50 62
⤷ pIC50 3.7 [62]
View species-specific antagonist tables
Antagonist Comments
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu5 (except for LY341495 value determined from functional studies). This is the only study describing affinity values for these compounds.

More information on agonist potencies determined from functional studies can be obtained from [83]. So far no differences have been reported for the antagonist affinities between the rat and the human receptor.

Surprisingly, although LY367385 and AIDA displace Quisqualate binding, no antagonistic activity of these compounds have been observed in functional studies (see [83]). (S)-4C3HPG has been reported to have slight partial agonist activity at this receptor [40].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0483605 Small molecule or natural product Rn Positive 6.5 pKB 35
⤷ pKB 6.5 [35]
GS39783 Small molecule or natural product Ligand has a PDB structure Rn Neutral 6.3 pKB 35
⤷ pKB 6.3 [35]
PHCCC Small molecule or natural product Click here for species-specific activity table Rn Neutral 5.6 pKB 35
⤷ pKB 5.6 [35]
AZ12216052 Small molecule or natural product Rn Positive 5.4 pKB 35
⤷ pKB 5.4 [35]
NPS 2143 Small molecule or natural product Rn Positive 5.1 pKB 35
⤷ pKB 5.1 [35]
CPCCOEt Small molecule or natural product Click here for species-specific activity table Rn Neutral 4.9 pKB 35
⤷ pKB 4.9 [35]
CGP7930 Small molecule or natural product Click here for species-specific activity table Rn Positive 4.8 pKB 35
⤷ pKB 4.8 [35]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.8 pKd 47
⤷ pKd 8.8 (Kd 1.5x10-9 M) [47]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.8 pKd 47
⤷ pKd 8.8 (Kd 1.7x10-9 M) [47]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Negative 8.7 pKd 47
⤷ pKd 8.7 (Kd 1.8x10-9 M) [47]
[3H]methoxy-PEPy Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.5 pKd 20
⤷ pKd 8.5 (Kd 3.4x10-9 M) [20]
[3H]methoxymethyl-MTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 7.7 pKd 20
⤷ pKd 7.7 (Kd 2x10-8 M) [20]
[3H]fenobam Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Negative 7.5 pKd 74
⤷ pKd 7.5 [74]
[3H]fenobam Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Negative 7.3 pKd 74
⤷ pKd 7.3 [74]
compound 20 [PMID: 16439120] Small molecule or natural product Rn Negative 9.0 pKi 13
⤷ pKi 9.0 (Ki 1x10-9 M) [13]
BOMA Small molecule or natural product Hs Negative 8.5 pKi 99
⤷ pKi 8.5 [99]
AZD9272 Small molecule or natural product Hs Negative 8.4 pKi 75
⤷ pKi 8.4 (Ki 3.8x10-9 M) [75]
GRN-529 Small molecule or natural product Rn Negative 8.3 pKi 38
⤷ pKi 8.3 (Ki 5.4x10-9 M) [38]
CTEP Small molecule or natural product Mm Negative 8.0 pKi 47
⤷ pKi 8.0 (Ki 9.5x10-9 M) [47]
compound 26 [PMID: 16439120] Small molecule or natural product Rn Negative 8.0 pKi 13
⤷ pKi 8.0 (Ki 1x10-8 M) [13]
compound 30 [PMID: 21757343] Small molecule or natural product Hs Negative 7.9 pKi 100
⤷ pKi 7.9 (Ki 1.2x10-8 M) [100]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 7.9 pKi 36
⤷ pKi 7.9 (Ki 1.2x10-8 M) [36]
CTEP Small molecule or natural product Rn Negative 7.9 pKi 47
⤷ pKi 7.9 (Ki 1.26x10-8 M) [47]
compound 8 [PMID: 15482908] Small molecule or natural product Rn Negative 7.8 pKi 89
⤷ pKi 7.8 (Ki 1.4x10-8 M) [89]
MTEP Small molecule or natural product Hs Negative 7.8 pKi 10
⤷ pKi 7.8 (Ki 1.6x10-8 M) [10]
VU0285683 Small molecule or natural product Rn Negative 7.8 pKi 76
⤷ pKi 7.8 (Ki 1.6x10-8 M) [76]
compound 29b [PMID: 20809633] Small molecule or natural product Rn Negative 7.8 pKi 12
⤷ pKi 7.8 (Ki 1.7x10-8 M) [12]
CTEP Small molecule or natural product Hs Negative 7.7 – 7.8 pKi 39,47
⤷ pKi 7.7 – 7.8 (Ki 2x10-8 – 1.64x10-8 M) [39,47]
compound 10 [PMID: 15482908] Small molecule or natural product Rn Negative 7.7 pKi 89
⤷ pKi 7.7 (Ki 1.9x10-8 M) [89]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 7.7 pKi 57
⤷ pKi 7.7 (Ki 2.2x10-8 M) [57]
AZD6538 Small molecule or natural product Hs Negative 7.6 pKi 75
⤷ pKi 7.6 (Ki 2.8x10-8 M) [75]
compound 24d [PMID: 23357634] Small molecule or natural product Rn Negative 7.5 pKi 106
⤷ pKi 7.5 (Ki 3x10-8 M) [106]
basimglurant Small molecule or natural product Hs Negative 7.4 pKi 39
⤷ pKi 7.4 (Ki 3.6x10-8 M) [39]
Description: Reduction of antagonist MPEP binding to mGlu5 receptors in vitro
compound 16m [PMID: 19931453] Small molecule or natural product Hs Negative 7.4 pKi 90
⤷ pKi 7.4 (Ki 3.8x10-8 M) [90]
VU0366058 Small molecule or natural product Rn Negative 7.1 pKi 61
⤷ pKi 7.1 (Ki 8.4x10-8 M) [61]
compound 16a [PMID: 14697765] Small molecule or natural product Rn Negative 7.0 pKi 99
⤷ pKi 7.0 (Ki 9.1x10-8 M) [99]
compound 42 [PMID: 17189691] Small molecule or natural product Rn Negative 7.0 pKi 14
⤷ pKi 7.0 (Ki 9.5x10-8 M) [14]
compound 8 [PMID: 20598884] Small molecule or natural product Rn Negative 7.0 pKi 25
⤷ pKi 7.0 (Ki 1.02x10-7 M) [25]
VU-1545 Small molecule or natural product Rn Positive 6.8 pKi 22
⤷ pKi 6.8 (Ki 1.56x10-7 M) [22]
compound 11a [PMID: 14697765] Small molecule or natural product Rn Negative 6.8 pKi 99
⤷ pKi 6.8 (Ki 1.59x10-7 M) [99]
VU0360172 Small molecule or natural product Rn Positive 6.7 pKi 76
⤷ pKi 6.7 (Ki 1.95x10-7 M) [76]
compound 27 [PMID: 20598884] Small molecule or natural product Rn Negative 6.7 pKi 25
⤷ pKi 6.7 (Ki 2.06x10-7 M) [25]
VU-29 Small molecule or natural product Rn Positive 6.6 pKi 16
⤷ pKi 6.6 (Ki 2.44x10-7 M) [16]
M-5MPEP Small molecule or natural product Rn Negative 6.5 pKi 77
⤷ pKi 6.5 (Ki 3x10-7 M) [77]
Br-5MPEPy Small molecule or natural product Rn Negative 6.5 pKi 77
⤷ pKi 6.5 (Ki 3x10-7 M) [77]
LSN2463359 Small molecule or natural product Rn Positive 6.4 pKi 31
⤷ pKi 6.4 (Ki 3.77x10-7 M) [31]
5-MPEP Small molecule or natural product Rn Neutral 6.4 pKi 77
⤷ pKi 6.4 [77]
compound 18 [PMID: 21927650] Small molecule or natural product Rn Negative 6.3 pKi 48
⤷ pKi 6.3 (Ki 4.77x10-7 M) [48]
LSN2814617 Small molecule or natural product Rn Positive 5.9 pKi 31
⤷ pKi 5.9 (Ki 1.34x10-6 M) [31]
5PAM523 Small molecule or natural product Rn Positive 5.7 pKi 68
⤷ pKi 5.7 (Ki 2x10-6 M) [68]
CPPZ Small molecule or natural product Rn Positive 5.5 pKi 91
⤷ pKi 5.5 (Ki 3.1x10-6 M) [91]
ADX-47273 Small molecule or natural product Rn Positive 5.4 pKi 31
⤷ pKi 5.4 (Ki 3.65x10-6 M) [31]
cinacalcet Small molecule or natural product Approved drug Rn Positive 4.3 pKi 35
⤷ pKi 4.3 [35]
VU0424465 Small molecule or natural product Rn Positive 8.8 pEC50 81
⤷ pEC50 8.8 (EC50 1.5x10-9 M) [81]
VU0404251 Small molecule or natural product Rn Positive 8.1 pEC50 54
⤷ pEC50 8.1 (EC50 7.2x10-9 M) [54]
VU-29 Small molecule or natural product Rn Positive 8.1 pEC50 16
⤷ pEC50 8.1 (EC50 9x10-9 M) [16]
VU-1545 Small molecule or natural product Hs Positive 8.0 pEC50 22
⤷ pEC50 8.0 (EC50 9.6x10-9 M) [22]
VU0463841 Small molecule or natural product Rn Negative 7.9 pEC50 2
⤷ pEC50 7.9 (EC50 1.3x10-8 M) [2]
compound 41 [PMID: 23434029] Small molecule or natural product Hs Negative 7.9 pEC50 15
⤷ pEC50 7.9 (EC50 1.3x10-8 M) [15]
CDPPB Small molecule or natural product Hs Positive 7.6 – 8.0 pEC50 44,49
⤷ pEC50 7.6 – 8.0 [44,49]
VU0360172 Small molecule or natural product Rn Positive 7.8 pEC50 76
⤷ pEC50 7.8 (EC50 1.6x10-8 M) [76]
CDPPB Small molecule or natural product Rn Positive 7.7 pEC50 49
⤷ pEC50 7.7 [49]
LSN2463359 Small molecule or natural product Rn Positive 7.6 pEC50 31
⤷ pEC50 7.6 (EC50 2.4x10-8 M) [31]
LSN2463359 Small molecule or natural product Hs Positive 7.5 pEC50 31
⤷ pEC50 7.5 (EC50 3.3x10-8 M) [31]
VU0357121 Small molecule or natural product Rn Positive 7.5 pEC50 32
⤷ pEC50 7.5 (EC50 3.3x10-8 M) [32]
VU0092273 Small molecule or natural product Rn Positive 7.5 pEC50 64
⤷ pEC50 7.5 (EC50 3.5x10-8 M) [64]
VU0240382 Small molecule or natural product Rn Positive 7.4 pEC50 64
⤷ pEC50 7.4 (EC50 3.9x10-8 M) [64]
compound 47 [PMID: 21295468] Small molecule or natural product Hs Positive 7.3 pEC50 96
⤷ pEC50 7.3 (EC50 5.01x10-8 M) [96]
LSN2814617 Small molecule or natural product Hs Positive 7.3 pEC50 31
⤷ pEC50 7.3 (EC50 5.2x10-8 M) [31]
ADX-47273 Small molecule or natural product Rn Positive 7.3 pEC50 31
⤷ pEC50 7.3 (EC50 5.5x10-8 M) [31]
VU0404251 Small molecule or natural product Hs Positive 7.2 pEC50 54
⤷ pEC50 7.2 (EC50 7x10-8 M) [54]
LSN2814617 Small molecule or natural product Rn Positive 7.0 pEC50 31
⤷ pEC50 7.0 (EC50 9.3x10-8 M) [31]
VU0361747 Small molecule or natural product Rn Positive 6.9 pEC50 64
⤷ pEC50 6.9 (EC50 1.26x10-7 M) [64]
ADX-47273 Small molecule or natural product Hs Positive 6.8 pEC50 31
⤷ pEC50 6.8 (EC50 1.57x10-7 M) [31]
5PAM523 Small molecule or natural product Hs Positive 6.7 pEC50 68
⤷ pEC50 6.7 (EC50 2.01x10-7 M) [68]
5PAM523 Small molecule or natural product Rn Positive 6.5 pEC50 68
⤷ pEC50 6.5 (EC50 3.11x10-7 M) [68]
NCFP Small molecule or natural product Rn Positive 6.0 – 6.7 pEC50 63
⤷ pEC50 6.7 (EC50 2.14x10-7 M) EC50 with high mGlu5 expression [63]
pEC50 6.4 (EC50 3.7x10-7 M) EC50 with low mGlu5 expression [63]
pEC50 6.0 (EC50 9.69x10-7 M) EC50 from assay using rat astrocytes [63]
CPPZ Small molecule or natural product Hs Positive 6.3 pEC50 91
⤷ pEC50 6.3 (EC50 5x10-7 M) [91]
VU0364289 Small molecule or natural product Rn Positive 5.8 pEC50 107
⤷ pEC50 5.8 (EC50 1.6x10-6 M) [107]
SP203 Small molecule or natural product Rn Negative 10.4 pIC50 87
⤷ pIC50 10.4 (IC50 3.6x10-11 M) [87]
compound 18 [PMID: 17723296] Small molecule or natural product Rn Negative 9.1 pIC50 101
⤷ pIC50 9.1 (IC50 7.2x10-10 M) [101]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 9.1 pIC50 57
⤷ pIC50 9.1 (IC50 8x10-10 M) [57]
MTEB Small molecule or natural product Hs Negative 8.7 pIC50 99
⤷ pIC50 8.7 [99]
GRN-529 Small molecule or natural product Hs Negative 8.6 pIC50 38
⤷ pIC50 8.6 (IC50 2.6x10-9 M) [38]
compound 8 [PMID: 15482908] Small molecule or natural product Hs Negative 8.4 pIC50 89
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [89]
[3H]M-MPEP Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Negative 8.3 – 8.4 pIC50 29,65
⤷ pIC50 8.4 [29]
pIC50 8.3 [65]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 8.2 pIC50 36
⤷ pIC50 8.2 (IC50 6.7x10-9 M) [36]
AZD9272 Small molecule or natural product Hs Negative 8.1 pIC50 75
⤷ pIC50 8.1 (IC50 7.6x10-9 M) [75]
alloswitch-1 Small molecule or natural product Primary target of this compound Rn Negative 8.1 pIC50 73
⤷ pIC50 8.1 (IC50 8.6x10-9 M) [73]
Description: Inhibition of agonist-induced IP accumulation.
CTEP Small molecule or natural product Hs Negative 7.9 – 8.2 pIC50 47
⤷ pIC50 7.9 – 8.2 (IC50 1.14x10-8 – 6.4x10-9 M) [47]
compound 30 [PMID: 21757343] Small molecule or natural product Rn Negative 7.9 pIC50 100
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [100]
VU0463841 Small molecule or natural product Rn Negative 7.9 pIC50 2
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [2]
AZD6538 Small molecule or natural product Hs Negative 7.9 pIC50 75
⤷ pIC50 7.9 (IC50 1.34x10-8 M) [75]
compound 29b [PMID: 20809633] Small molecule or natural product Hs Negative 7.8 pIC50 12
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [12]
compound 30 [PMID: 21757343] Small molecule or natural product Hs Negative 7.8 pIC50 100
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [100]
compound 24 [PMID: 23374867] Small molecule or natural product Hs Negative 7.7 pIC50 33
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [33]
[14C]MTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 7.7 pIC50 3
⤷ pIC50 7.7 [3]
dipraglurant Small molecule or natural product Hs Negative 7.7 pIC50 15
⤷ pIC50 7.7 (IC50 2x10-8 M) [15]
compound 16a [PMID: 14697765] Small molecule or natural product Hs Negative 7.7 pIC50 99
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [99]
compound 24d [PMID: 23357634] Small molecule or natural product Hs Negative 7.6 pIC50 106
⤷ pIC50 7.6 (IC50 2.3x10-8 M) [106]
VU0285683 Small molecule or natural product Rn Negative 7.6 pIC50 76
⤷ pIC50 7.6 (IC50 2.44x10-8 M) [76]
MPEP Small molecule or natural product Click here for species-specific activity table Hs Negative 7.4 – 7.7 pIC50 29-30
⤷ pIC50 7.4 – 7.7 [29-30]
compound 13 [PMID: 15686941] Small molecule or natural product Hs Negative 7.6 pIC50 6
⤷ pIC50 7.6 (IC50 2.8x10-8 M) [6]
methoxymethyl-MTEP Small molecule or natural product Rn Negative 7.5 pIC50 3
⤷ pIC50 7.5 (IC50 3x10-8 M) [3]
compound 16m [PMID: 19931453] Small molecule or natural product Hs Negative 7.5 pIC50 90
⤷ pIC50 7.5 (IC50 3.2x10-8 M) [90]
compound 11a [PMID: 14697765] Small molecule or natural product Hs Negative 7.4 pIC50 99
⤷ pIC50 7.4 (IC50 4.1x10-8 M) [99]
GSK2210875 Small molecule or natural product Hs Negative 7.4 pIC50 70
⤷ pIC50 7.4 (IC50 4x10-8 M) [70]
compound