Details of the Target
General Information of Target
Target ID | LDTP11366 | |||||
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Target Name | Leucine-rich repeat-containing G-protein coupled receptor 4 (LGR4) | |||||
Gene Name | LGR4 | |||||
Gene ID | 55366 | |||||
Synonyms |
GPR48; Leucine-rich repeat-containing G-protein coupled receptor 4; G-protein coupled receptor 48 |
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3D Structure | ||||||
Sequence |
MDDAAVLKRRGYLLGINLGEGSYAKVKSAYSERLKFNVAIKIIDRKKAPADFLEKFLPRE
IEILAMLNHCSIIKTYEIFETSHGKVYIVMELAVQGDLLELIKTRGALHEDEARKKFHQL SLAIKYCHDLDVVHRDLKCDNLLLDKDFNIKLSDFSFSKRCLRDDSGRMALSKTFCGSPA YAAPEVLQGIPYQPKVYDIWSLGVILYIMVCGSMPYDDSNIKKMLRIQKEHRVNFPRSKH LTGECKDLIYHMLQPDVNRRLHIDEILSHCWMQPKARGSPSVAINKEGESSRGTEPLWTP EPGSDKKSATKLEPEGEAQPQAQPETKPEGTAMQMSRQSEILGFPSKPSTMETEEGPPQQ PPETRAQ |
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Target Type |
Preclinical
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Target Bioclass |
GPCR
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Family |
G-protein coupled receptor 1 family
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Subcellular location |
Cell membrane
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Function |
Receptor for R-spondins that potentiates the canonical Wnt signaling pathway and is involved in the formation of various organs. Upon binding to R-spondins (RSPO1, RSPO2, RSPO3 or RSPO4), associates with phosphorylated LRP6 and frizzled receptors that are activated by extracellular Wnt receptors, triggering the canonical Wnt signaling pathway to increase expression of target genes. In contrast to classical G-protein coupled receptors, does not activate heterotrimeric G-proteins to transduce the signal. Its function as activator of the Wnt signaling pathway is required for the development of various organs, including liver, kidney, intestine, bone, reproductive tract and eye. May also act as a receptor for norrin (NDP), such results however require additional confirmation in vivo. Required during spermatogenesis to activate the Wnt signaling pathway in peritubular myoid cells. Required for the maintenance of intestinal stem cells and Paneth cell differentiation in postnatal intestinal crypts. Acts as a regulator of bone formation and remodeling. Involved in kidney development; required for maintaining the ureteric bud in an undifferentiated state. Involved in the development of the anterior segment of the eye. Required during erythropoiesis. Also acts as a negative regulator of innate immunity by inhibiting TLR2/TLR4 associated pattern-recognition and pro-inflammatory cytokine production. Plays an important role in regulating the circadian rhythms of plasma lipids, partially through regulating the rhythmic expression of MTTP. Required for proper development of GnRH neurons (gonadotropin-releasing hormone expressing neurons) that control the release of reproductive hormones from the pituitary gland.
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TTD ID | ||||||
Uniprot ID | ||||||
DrugMap ID | ||||||
Ensemble ID | ||||||
HGNC ID |
Target Site Mutations in Different Cell Lines
Probe(s) Labeling This Target
ABPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
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DBIA Probe Info |
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C930(1.78) | LDD3367 | [1] | |
IPM Probe Info |
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N.A. | LDD0147 | [2] |
Competitor(s) Related to This Target
Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
---|---|---|---|---|---|
LDCM0214 | AC1 | HEK-293T | C930(1.04) | LDD1507 | [3] |
LDCM0215 | AC10 | HEK-293T | C930(1.09) | LDD1508 | [3] |
LDCM0237 | AC12 | HEK-293T | C339(1.02); C930(0.94) | LDD1510 | [3] |
LDCM0259 | AC14 | HEK-293T | C930(0.97) | LDD1512 | [3] |
LDCM0270 | AC15 | HEK-293T | C930(1.06) | LDD1513 | [3] |
LDCM0276 | AC17 | HEK-293T | C930(1.05) | LDD1515 | [3] |
LDCM0277 | AC18 | HEK-293T | C930(1.04) | LDD1516 | [3] |
LDCM0279 | AC2 | HEK-293T | C930(1.08) | LDD1518 | [3] |
LDCM0280 | AC20 | HEK-293T | C339(1.04); C930(0.95) | LDD1519 | [3] |
LDCM0281 | AC21 | HEK-293T | C930(0.92) | LDD1520 | [3] |
LDCM0282 | AC22 | HEK-293T | C930(0.89) | LDD1521 | [3] |
LDCM0283 | AC23 | HEK-293T | C930(0.96) | LDD1522 | [3] |
LDCM0284 | AC24 | HEK-293T | C930(0.98) | LDD1523 | [3] |
LDCM0285 | AC25 | HEK-293T | C930(1.08) | LDD1524 | [3] |
LDCM0286 | AC26 | HEK-293T | C930(1.10) | LDD1525 | [3] |
LDCM0288 | AC28 | HEK-293T | C339(1.04); C930(1.01) | LDD1527 | [3] |
LDCM0289 | AC29 | HEK-293T | C930(0.92) | LDD1528 | [3] |
LDCM0291 | AC30 | HEK-293T | C930(1.00) | LDD1530 | [3] |
LDCM0292 | AC31 | HEK-293T | C930(0.97) | LDD1531 | [3] |
LDCM0293 | AC32 | HEK-293T | C930(0.98) | LDD1532 | [3] |
LDCM0294 | AC33 | HEK-293T | C930(1.02) | LDD1533 | [3] |
LDCM0295 | AC34 | HEK-293T | C930(1.06) | LDD1534 | [3] |
LDCM0297 | AC36 | HEK-293T | C339(1.10); C930(0.94) | LDD1536 | [3] |
LDCM0298 | AC37 | HEK-293T | C930(0.96) | LDD1537 | [3] |
LDCM0299 | AC38 | HEK-293T | C930(0.92) | LDD1538 | [3] |
LDCM0300 | AC39 | HEK-293T | C930(1.01) | LDD1539 | [3] |
LDCM0301 | AC4 | HEK-293T | C339(1.04); C930(1.02) | LDD1540 | [3] |
LDCM0302 | AC40 | HEK-293T | C930(0.96) | LDD1541 | [3] |
LDCM0303 | AC41 | HEK-293T | C930(1.09) | LDD1542 | [3] |
LDCM0304 | AC42 | HEK-293T | C930(1.14) | LDD1543 | [3] |
LDCM0306 | AC44 | HEK-293T | C339(1.03); C930(1.01) | LDD1545 | [3] |
LDCM0307 | AC45 | HEK-293T | C930(0.97) | LDD1546 | [3] |
LDCM0308 | AC46 | HEK-293T | C930(1.04) | LDD1547 | [3] |
LDCM0309 | AC47 | HEK-293T | C930(0.99) | LDD1548 | [3] |
LDCM0310 | AC48 | HEK-293T | C930(0.98) | LDD1549 | [3] |
LDCM0311 | AC49 | HEK-293T | C930(0.94) | LDD1550 | [3] |
LDCM0312 | AC5 | HEK-293T | C930(1.16) | LDD1551 | [3] |
LDCM0313 | AC50 | HEK-293T | C930(1.07) | LDD1552 | [3] |
LDCM0315 | AC52 | HEK-293T | C339(1.04); C930(1.00) | LDD1554 | [3] |
LDCM0316 | AC53 | HEK-293T | C930(1.00) | LDD1555 | [3] |
LDCM0317 | AC54 | HEK-293T | C930(1.08) | LDD1556 | [3] |
LDCM0318 | AC55 | HEK-293T | C930(0.97) | LDD1557 | [3] |
LDCM0319 | AC56 | HEK-293T | C930(0.93) | LDD1558 | [3] |
LDCM0320 | AC57 | HEK-293T | C930(1.03) | LDD1559 | [3] |
LDCM0321 | AC58 | HEK-293T | C930(1.04) | LDD1560 | [3] |
LDCM0323 | AC6 | HEK-293T | C930(1.01) | LDD1562 | [3] |
LDCM0324 | AC60 | HEK-293T | C339(1.05); C930(0.96) | LDD1563 | [3] |
LDCM0325 | AC61 | HEK-293T | C930(1.03) | LDD1564 | [3] |
LDCM0326 | AC62 | HEK-293T | C930(1.00) | LDD1565 | [3] |
LDCM0327 | AC63 | HEK-293T | C930(1.06) | LDD1566 | [3] |
LDCM0328 | AC64 | HEK-293T | C930(1.00) | LDD1567 | [3] |
LDCM0334 | AC7 | HEK-293T | C930(1.04) | LDD1568 | [3] |
LDCM0345 | AC8 | HEK-293T | C930(0.92) | LDD1569 | [3] |
LDCM0248 | AKOS034007472 | HEK-293T | C930(1.03) | LDD1511 | [3] |
LDCM0356 | AKOS034007680 | HEK-293T | C930(1.14) | LDD1570 | [3] |
LDCM0275 | AKOS034007705 | HEK-293T | C930(1.00) | LDD1514 | [3] |
LDCM0367 | CL1 | HEK-293T | C930(1.11) | LDD1571 | [3] |
LDCM0368 | CL10 | HEK-293T | C930(1.17) | LDD1572 | [3] |
LDCM0369 | CL100 | HEK-293T | C930(1.02) | LDD1573 | [3] |
LDCM0370 | CL101 | HEK-293T | C930(0.98) | LDD1574 | [3] |
LDCM0371 | CL102 | HEK-293T | C930(1.25) | LDD1575 | [3] |
LDCM0372 | CL103 | HEK-293T | C930(1.03) | LDD1576 | [3] |
LDCM0373 | CL104 | HEK-293T | C930(0.99) | LDD1577 | [3] |
LDCM0374 | CL105 | HEK-293T | C930(0.91) | LDD1578 | [3] |
LDCM0375 | CL106 | HEK-293T | C930(1.01) | LDD1579 | [3] |
LDCM0376 | CL107 | HEK-293T | C930(0.90) | LDD1580 | [3] |
LDCM0377 | CL108 | HEK-293T | C930(1.07) | LDD1581 | [3] |
LDCM0378 | CL109 | HEK-293T | C930(1.07) | LDD1582 | [3] |
LDCM0379 | CL11 | HEK-293T | C930(1.05) | LDD1583 | [3] |
LDCM0380 | CL110 | HEK-293T | C930(1.20) | LDD1584 | [3] |
LDCM0381 | CL111 | HEK-293T | C930(0.94) | LDD1585 | [3] |
LDCM0382 | CL112 | HEK-293T | C930(0.98) | LDD1586 | [3] |
LDCM0383 | CL113 | HEK-293T | C930(1.03) | LDD1587 | [3] |
LDCM0384 | CL114 | HEK-293T | C930(1.19) | LDD1588 | [3] |
LDCM0385 | CL115 | HEK-293T | C930(0.84) | LDD1589 | [3] |
LDCM0386 | CL116 | HEK-293T | C930(1.17) | LDD1590 | [3] |
LDCM0387 | CL117 | HEK-293T | C930(1.07) | LDD1591 | [3] |
LDCM0388 | CL118 | HEK-293T | C930(1.15) | LDD1592 | [3] |
LDCM0389 | CL119 | HEK-293T | C930(0.98) | LDD1593 | [3] |
LDCM0390 | CL12 | HEK-293T | C930(1.14) | LDD1594 | [3] |
LDCM0391 | CL120 | HEK-293T | C930(1.04) | LDD1595 | [3] |
LDCM0392 | CL121 | HEK-293T | C930(1.01) | LDD1596 | [3] |
LDCM0393 | CL122 | HEK-293T | C930(1.15) | LDD1597 | [3] |
LDCM0394 | CL123 | HEK-293T | C930(1.12) | LDD1598 | [3] |
LDCM0395 | CL124 | HEK-293T | C930(1.06) | LDD1599 | [3] |
LDCM0396 | CL125 | HEK-293T | C930(1.09) | LDD1600 | [3] |
LDCM0397 | CL126 | HEK-293T | C930(1.05) | LDD1601 | [3] |
LDCM0398 | CL127 | HEK-293T | C930(1.02) | LDD1602 | [3] |
LDCM0399 | CL128 | HEK-293T | C930(1.03) | LDD1603 | [3] |
LDCM0400 | CL13 | HEK-293T | C930(1.02) | LDD1604 | [3] |
LDCM0401 | CL14 | HEK-293T | C930(1.08) | LDD1605 | [3] |
LDCM0402 | CL15 | HEK-293T | C930(1.03) | LDD1606 | [3] |
LDCM0403 | CL16 | HEK-293T | C930(1.10) | LDD1607 | [3] |
LDCM0404 | CL17 | HEK-293T | C930(1.14) | LDD1608 | [3] |
LDCM0405 | CL18 | HEK-293T | C930(1.03) | LDD1609 | [3] |
LDCM0407 | CL2 | HEK-293T | C930(1.02) | LDD1611 | [3] |
LDCM0408 | CL20 | HEK-293T | C339(1.17); C930(0.95) | LDD1612 | [3] |
LDCM0409 | CL21 | HEK-293T | C930(1.14) | LDD1613 | [3] |
LDCM0410 | CL22 | HEK-293T | C930(1.07) | LDD1614 | [3] |
LDCM0411 | CL23 | HEK-293T | C930(1.01) | LDD1615 | [3] |
LDCM0412 | CL24 | HEK-293T | C930(1.16) | LDD1616 | [3] |
LDCM0413 | CL25 | HEK-293T | C930(1.04) | LDD1617 | [3] |
LDCM0414 | CL26 | HEK-293T | C930(1.19) | LDD1618 | [3] |
LDCM0415 | CL27 | HEK-293T | C930(0.85) | LDD1619 | [3] |
LDCM0416 | CL28 | HEK-293T | C930(1.05) | LDD1620 | [3] |
LDCM0417 | CL29 | HEK-293T | C930(1.17) | LDD1621 | [3] |
LDCM0418 | CL3 | HEK-293T | C930(0.98) | LDD1622 | [3] |
LDCM0419 | CL30 | HEK-293T | C930(1.06) | LDD1623 | [3] |
LDCM0421 | CL32 | HEK-293T | C339(1.18); C930(1.06) | LDD1625 | [3] |
LDCM0422 | CL33 | HEK-293T | C930(1.31) | LDD1626 | [3] |
LDCM0423 | CL34 | HEK-293T | C930(1.09) | LDD1627 | [3] |
LDCM0424 | CL35 | HEK-293T | C930(1.12) | LDD1628 | [3] |
LDCM0425 | CL36 | HEK-293T | C930(1.07) | LDD1629 | [3] |
LDCM0426 | CL37 | HEK-293T | C930(0.90) | LDD1630 | [3] |
LDCM0428 | CL39 | HEK-293T | C930(0.99) | LDD1632 | [3] |
LDCM0429 | CL4 | HEK-293T | C930(1.05) | LDD1633 | [3] |
LDCM0430 | CL40 | HEK-293T | C930(1.06) | LDD1634 | [3] |
LDCM0431 | CL41 | HEK-293T | C930(1.09) | LDD1635 | [3] |
LDCM0432 | CL42 | HEK-293T | C930(1.11) | LDD1636 | [3] |
LDCM0434 | CL44 | HEK-293T | C339(1.14); C930(1.09) | LDD1638 | [3] |
LDCM0435 | CL45 | HEK-293T | C930(1.10) | LDD1639 | [3] |
LDCM0436 | CL46 | HEK-293T | C930(1.08) | LDD1640 | [3] |
LDCM0437 | CL47 | HEK-293T | C930(1.10) | LDD1641 | [3] |
LDCM0438 | CL48 | HEK-293T | C930(1.08) | LDD1642 | [3] |
LDCM0439 | CL49 | HEK-293T | C930(0.93) | LDD1643 | [3] |
LDCM0440 | CL5 | HEK-293T | C930(0.94) | LDD1644 | [3] |
LDCM0441 | CL50 | HEK-293T | C930(1.19) | LDD1645 | [3] |
LDCM0443 | CL52 | HEK-293T | C930(1.10) | LDD1646 | [3] |
LDCM0444 | CL53 | HEK-293T | C930(1.23) | LDD1647 | [3] |
LDCM0445 | CL54 | HEK-293T | C930(1.31) | LDD1648 | [3] |
LDCM0447 | CL56 | HEK-293T | C339(1.11); C930(1.13) | LDD1650 | [3] |
LDCM0448 | CL57 | HEK-293T | C930(1.21) | LDD1651 | [3] |
LDCM0449 | CL58 | HEK-293T | C930(1.11) | LDD1652 | [3] |
LDCM0450 | CL59 | HEK-293T | C930(1.09) | LDD1653 | [3] |
LDCM0451 | CL6 | HEK-293T | C930(1.17) | LDD1654 | [3] |
LDCM0452 | CL60 | HEK-293T | C930(1.00) | LDD1655 | [3] |
LDCM0453 | CL61 | HEK-293T | C930(1.02) | LDD1656 | [3] |
LDCM0454 | CL62 | HEK-293T | C930(1.06) | LDD1657 | [3] |
LDCM0455 | CL63 | HEK-293T | C930(0.92) | LDD1658 | [3] |
LDCM0456 | CL64 | HEK-293T | C930(1.17) | LDD1659 | [3] |
LDCM0457 | CL65 | HEK-293T | C930(1.10) | LDD1660 | [3] |
LDCM0458 | CL66 | HEK-293T | C930(1.17) | LDD1661 | [3] |
LDCM0460 | CL68 | HEK-293T | C339(1.09); C930(1.14) | LDD1663 | [3] |
LDCM0461 | CL69 | HEK-293T | C930(1.05) | LDD1664 | [3] |
LDCM0463 | CL70 | HEK-293T | C930(1.00) | LDD1666 | [3] |
LDCM0464 | CL71 | HEK-293T | C930(1.13) | LDD1667 | [3] |
LDCM0465 | CL72 | HEK-293T | C930(1.18) | LDD1668 | [3] |
LDCM0466 | CL73 | HEK-293T | C930(0.97) | LDD1669 | [3] |
LDCM0467 | CL74 | HEK-293T | C930(1.21) | LDD1670 | [3] |
LDCM0469 | CL76 | HEK-293T | C930(0.99) | LDD1672 | [3] |
LDCM0470 | CL77 | HEK-293T | C930(1.13) | LDD1673 | [3] |
LDCM0471 | CL78 | HEK-293T | C930(1.05) | LDD1674 | [3] |
LDCM0473 | CL8 | HEK-293T | C339(1.09); C930(1.43) | LDD1676 | [3] |
LDCM0474 | CL80 | HEK-293T | C339(1.07); C930(0.95) | LDD1677 | [3] |
LDCM0475 | CL81 | HEK-293T | C930(0.98) | LDD1678 | [3] |
LDCM0476 | CL82 | HEK-293T | C930(1.07) | LDD1679 | [3] |
LDCM0477 | CL83 | HEK-293T | C930(1.12) | LDD1680 | [3] |
LDCM0478 | CL84 | HEK-293T | C930(1.13) | LDD1681 | [3] |
LDCM0479 | CL85 | HEK-293T | C930(0.94) | LDD1682 | [3] |
LDCM0480 | CL86 | HEK-293T | C930(1.12) | LDD1683 | [3] |
LDCM0481 | CL87 | HEK-293T | C930(0.95) | LDD1684 | [3] |
LDCM0482 | CL88 | HEK-293T | C930(0.92) | LDD1685 | [3] |
LDCM0483 | CL89 | HEK-293T | C930(1.00) | LDD1686 | [3] |
LDCM0484 | CL9 | HEK-293T | C930(1.03) | LDD1687 | [3] |
LDCM0485 | CL90 | HEK-293T | C930(1.50) | LDD1688 | [3] |
LDCM0487 | CL92 | HEK-293T | C339(1.11); C930(1.08) | LDD1690 | [3] |
LDCM0488 | CL93 | HEK-293T | C930(1.08) | LDD1691 | [3] |
LDCM0489 | CL94 | HEK-293T | C930(1.07) | LDD1692 | [3] |
LDCM0490 | CL95 | HEK-293T | C930(1.31) | LDD1693 | [3] |
LDCM0491 | CL96 | HEK-293T | C930(1.00) | LDD1694 | [3] |
LDCM0492 | CL97 | HEK-293T | C930(1.04) | LDD1695 | [3] |
LDCM0493 | CL98 | HEK-293T | C930(1.05) | LDD1696 | [3] |
LDCM0494 | CL99 | HEK-293T | C930(0.87) | LDD1697 | [3] |
LDCM0495 | E2913 | HEK-293T | C930(1.06) | LDD1698 | [3] |
LDCM0468 | Fragment33 | HEK-293T | C930(0.89) | LDD1671 | [3] |
LDCM0427 | Fragment51 | HEK-293T | C930(1.14) | LDD1631 | [3] |
LDCM0022 | KB02 | HEK-293T | C930(0.90); C339(1.11) | LDD1492 | [3] |
LDCM0023 | KB03 | HEK-293T | C930(0.99); C339(0.97) | LDD1497 | [3] |
LDCM0024 | KB05 | NUGC-3 | C930(1.78) | LDD3367 | [1] |
The Interaction Atlas With This Target
References