Development Level

Tclin 127,635 | 130,166
Tchem 103,291 | 105,938

Target Family

Enzyme 84,848 | 85,645
GPCR 57,281 | 59,407
Kinase 33,192 | 33,996
Ion Channel 16,370 | 16,788
Non-IDG 16,060 | 16,175
Transporter 9,069 | 9,204
Nuclear Receptor 7,012 | 7,246
Epigenetic 4,980 | 5,140
Transcription Factor 405 | 410
TF/Epigenetic 98 | 108

Target

KCNH2 4,421 | 4,432
CA2 4,185 | 4,185
F10 3,874 | 3,879
BACE1 3,667 | 3,691
SLC6A4 3,422 | 3,433
DPP4 3,096 | 3,107
SCN9A 2,962 | 2,970
F2 2,715 | 2,721
PDE10A 2,699 | 2,702
CA1 2,648 | 2,654
HSD11B1 2,490 | 2,493
CA9 2,402 | 2,402
DRD2 2,394 | 2,432
DRD3 2,378 | 2,406
REN 2,302 | 2,303
MAPT 2,286 | 2,286
HDAC1 2,256 | 2,280
MMP2 2,243 | 2,249
HRH3 2,232 | 2,278
SLC6A2 2,218 | 2,227
HTR1A 2,144 | 2,209
HTR2A 2,030 | 2,122
MMP13 2,029 | 2,036
MCHR1 2,026 | 2,039
CA12 2,005 | 2,010
HTR6 1,960 | 2,009
ACACB 1,928 | 1,930
CNR2 1,909 | 1,926
ACHE 1,869 | 1,877
ALOX5AP 1,860 | 1,860
SIGMAR1 1,846 | 1,854
TACR1 1,832 | 1,853
MMP9 1,826 | 1,834
OPRM1 1,778 | 1,833
SLC6A3 1,758 | 1,766
MTOR 1,724 | 1,755
ADORA3 1,693 | 1,774
KDR 1,658 | 1,715
OPRK1 1,631 | 1,683
PARP1 1,625 | 1,628
OPRD1 1,563 | 1,607
CTSS 1,561 | 1,565
PTGS2 1,554 | 1,569
CNR1 1,518 | 1,548
ADORA2A 1,512 | 1,585
NR3C1 1,481 | 1,509
MDM2 1,448 | 1,448
MMP1 1,448 | 1,452
EGFR 1,401 | 1,445
P2RX7 1,398 | 1,410
TRPV1 1,397 | 1,427
CTSK 1,395 | 1,400
EPHX2 1,371 | 1,376
HDAC6 1,367 | 1,390
MMP3 1,342 | 1,345
MAPK14 1,321 | 1,345
JAK2 1,320 | 1,350
PIK3CA 1,314 | 1,366
PTGDR2 1,310 | 1,332
DRD4 1,285 | 1,320
MET 1,250 | 1,273
CCR5 1,186 | 1,197
ADAM17 1,185 | 1,190
HTR2C 1,173 | 1,221
CRHR1 1,161 | 1,163
CYP19A1 1,135 | 1,140
PIM1 1,123 | 1,138
PDE5A 1,111 | 1,120
ADORA1 1,102 | 1,178
JAK1 1,070 | 1,095
MAOB 1,060 | 1,065
MC4R 1,050 | 1,053
ADRA1A 1,032 | 1,054
BRAF 1,007 | 1,020
ELANE 973 | 979
ESR1 953 | 967
OPRL1 945 | 958
SLC5A2 945 | 950
PPARG 935 | 980
HTR7 931 | 976
BCL2 930 | 932
ESR2 909 | 923
CHRM3 901 | 950
FAAH 900 | 912
MMP8 874 | 878
AURKA 870 | 898
SYK 848 | 864
CHEK1 847 | 863
HCRTR2 838 | 854
ADORA2B 836 | 900
CCR2 829 | 843
P2RX3 823 | 830
BCHE 814 | 816
PDE4B 805 | 813
PRSS1 790 | 792
HTR1D 786 | 824
S1PR1 786 | 810
TDP1 782 | 782
AR 781 | 796
CTSL 776 | 778

Pharmalogical Action

INHIBITOR 527 | 542
AGONIST 415 | 427
ANTAGONIST 345 | 350
BLOCKER 124 | 129
ANTIBODY BINDING 57 | 57
POSITIVE ALLOSTERIC MODULATOR 51 | 51
ACTIVATOR 28 | 30
MODULATOR 20 | 20
OPENER 16 | 16
POSITIVE MODULATOR 15 | 15
PARTIAL AGONIST 14 | 14
INVERSE AGONIST 8 | 9
GATING INHIBITOR 6 | 6
NEGATIVE ALLOSTERIC MODULATOR 5 | 5
RELEASING AGENT 5 | 5
SUBSTRATE 5 | 5
ALLOSTERIC MODULATOR 3 | 4
PHARMACOLOGICAL CHAPERONE 3 | 3
ALLOSTERIC ANTAGONIST 2 | 2
OTHER 1 | 1

Ligand Activity

IC50 141,198 | 143,077
Ki 69,926 | 70,819
EC50 7,789 | 8,212
Potency 2,975 | 2,975
Kd 2,659 | 2,908
AC50 517 | 517
- 88 | 698
KB 1 | 17

Ligand Activity Source

ChEMBL 220,945 | 220,950
Guide to Pharmacology 369 | 5,022

Ligand Source

CHEMBL 221,632 | 221,632
Guide to Pharmacology 369 | 5,022
SCIENTIFIC LITERATURE 253 | 269
DRUG LABEL 240 | 243
IUPHAR 109 | 129
KEGG DRUG 43 | 45